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Ernest Hamel

Research Profile

Chemicals & Drugs

Anatomy

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Procedures

Drug Screening Assays, Antitumor

Physiology

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Publications

TOP 3
Romeo Romagnoli; Mojgan Aghazadeh Tabrizi; Pier Giovanni Baraldi; Marcella Bassetto; Giuseppe Basso; Roberta Bortolozzi; Andrea Brancale; Ignazio Castagliuolo; Ernest Hamel; Maria Kimatrai Salvador; Delia Preti; Giampietro Viola
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
Romeo Romagnoli; Maria Kimatrai Salvador; Mojgan Aghazadeh Tabrizi; Pier Giovanni Baraldi; Marcella Bassetto; Giuseppe Basso; Roberta Bortolozzi; Andrea Brancale; M Encarnacion Camacho; Ernest Hamel; Delia Preti; Giampietro Viola
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
Taradas Sarkar; Zhi-Wei Su; Ruoli Bai; Rick Gussio; Jun Hao; Tam Luong Nguyen; Samuel X Qiu; Ernest Hamel
Interaction of pseudolaric acid B with the colchicine site of tubulin.

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All Publications

2013: Romeo Romagnoli; Mojgan Aghazadeh Tabrizi; Pier Giovanni Baraldi; Marcella Bassetto; Giuseppe Basso; Roberta Bortolozzi; Andrea Brancale; Ignazio Castagliuolo; Ernest Hamel; Maria Kimatrai Salvador; Delia Preti; Giampietro Viola
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
Journal of medicinal chemistry 2013;56(6):2606-18.
2012: Romeo Romagnoli; Maria Kimatrai Salvador; Mojgan Aghazadeh Tabrizi; Pier Giovanni Baraldi; Marcella Bassetto; Giuseppe Basso; Roberta Bortolozzi; Andrea Brancale; M Encarnacion Camacho; Ernest Hamel; Delia Preti; Giampietro Viola
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
Bioorganic & medicinal chemistry 2012;20(24):7083-94.
2012: Taradas Sarkar; Zhi-Wei Su; Ruoli Bai; Rick Gussio; Jun Hao; Tam Luong Nguyen; Samuel X Qiu; Ernest Hamel
Interaction of pseudolaric acid B with the colchicine site of tubulin.
Biochemical pharmacology 2012;84(4):444-50.
2012: Romeo Romagnoli; Maria Kimatrai Salvador; Su-zhan Zhang; Mojgan Aghazadeh Tabrizi; Pier Giovanni Baraldi; Giuseppe Basso; Roberta Bortolozzi; Andrea Brancale; Xian-Hua Fu; Ernest Hamel; Jun Li; Elena Porcù; Delia Preti; Giampietro Viola
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
Journal of medicinal chemistry 2012;55(11):5433-45.
2011: Romeo Romagnoli; Giampietro Viola; Su-zhan Zhang; Maria Kimatrai Salvador; Jun Li; LUISA-CARLOTA LÓPEZ-CARA; Jan Balzarini; Pier Giovanni Baraldi; Giuseppe Basso; Roberta Bortolozzi; Andrea Brancale; Xian-Hua Fu; Ernest Hamel
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
European journal of medicinal chemistry 2011;46(12):6015-24.
2011: Romeo Romagnoli; Jae Gwan Kim; Maria Kimatrai Salvador; LUISA-CARLOTA LÓPEZ-CARA; Antonio Ricci; Jan Balzarini; Pier Giovanni Baraldi; Jaime Bermejo; Andrea Brancale; Maria Dora Carrion; Longchuan Chen; Olga Cruz-Lopez; Francisco Estévez; Sara Estévez; Ernest Hamel
Synthesis and antitumor molecular mechanism of agents based on amino 2-(3',4',5'-trimethoxybenzoyl)benzo[b]furan: inhibition of tubulin and induction of apoptosis.
ChemMedChem 2011;6(10):1841-53.
2011: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Giuseppe Basso; Roberta Bortolozzi; Andrea Brancale; Ernest Hamel; Antonio Ricci; Giampietro Viola
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
Journal of medicinal chemistry 2011;54(14):5144-53.
2011: Ruoli Bai; James C Burnett; Rick Gussio; Murray H G Munro; Tam Luong Nguyen; George R Pettit; Amos B Smith; Onur Atasoylu; Ernest Hamel
Interactions of halichondrin B and eribulin with tubulin.
Journal of chemical information and modeling 2011;51(6):1393-404.
2011: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Olga Cruz-Lopez; Manlio Tolomeo; Rosaria Maria Pipitone; Stefania Grimaudo; Jan Balzarini; Andrea Brancale; Antonietta Di Cristina; Ernest Hamel
Synthesis of novel antimitotic agents based on 2-amino-3-aroyl-5-(hetero)arylethynyl thiophene derivatives.
Bioorganic & medicinal chemistry letters 2011;21(9):2746-51.
2010: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Carlota Lopez Cara; Ernest Hamel; Giuseppe Basso; Roberta Bortolozzi; Giampietro Viola
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-aryl/arylaminobenzo[b]thiophene derivatives as a novel class of antiproliferative agents.
European journal of medicinal chemistry 2010;45(12):5781-91.
2010: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Maria Giovanna Pavani; Olga Cruz-Lopez; Ernest Hamel; Jan Balzarini; Eleonora Brognara; Cristina Zuccato; Roberto Gambari
Synthesis and cellular pharmacology studies of a series of 2-amino-3-aroyl-4-substituted thiophene derivatives.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2010;6(6):329-43.
2010: Arun K Ghosh; Zachary L Dawson; Deuk Kyu Moon; Ruoli Bai; Ernest Hamel
Synthesis and biological evaluation of new jasplakinolide (jaspamide) analogs.
Bioorganic & medicinal chemistry letters 2010;20(17):5104-7.
2010: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Maria Dora Carrion; Olga Cruz-Lopez; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Maria Rosaria Pipitone; Jan Balzarini; Andrea Brancale; Ernest Hamel
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
Bioorganic & medicinal chemistry 2010;18(14):5114-22.
2010: Romeo Romagnoli; Pier Giovanni Baraldi; Olga Cruz-Lopez; LUISA-CARLOTA LÓPEZ-CARA; Maria Dora Carrion; Andrea Brancale; Ernest Hamel; Longchuan Chen; Roberta Bortolozzi; Giuseppe Basso; Giampietro Viola
Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.
Journal of medicinal chemistry 2010;53(10):4248-58.
2010: Romeo Romagnoli; Pier Giovanni Baraldi; Olga Cruz-Lopez; LUISA-CARLOTA LÓPEZ-CARA; Maria Dora Carrion; Jan Balzarini; Ernest Hamel; Giuseppe Basso; Roberta Bortolozzi; Giampietro Viola
Symmetrical alpha-bromoacryloylamido diaryldienone derivatives as a novel series of antiproliferative agents. Design, synthesis and biological evaluation.
Bioorganic & medicinal chemistry letters 2010;20(9):2733-9.
2009: Giuseppe La Regina; Taradas Sarkar; Ruoli Bai; Michael Edler; Roberto Saletti; Antonio Coluccia; Francesco Piscitelli; Lara Minelli; Valerio Gatti; Carmela Mazzoccoli; Vanessa Palermo; cristina mazzoni; Claudio Falcone; Anna Scovassi; Vincenzo Giansanti; Pietro Campiglia; Amalia Porta; Bruno Maresca; Ernest Hamel; Andrea Brancale; Ettore Novellino; Romano Silvestri
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
Journal of medicinal chemistry 2009;52(23):7512-27.
2009: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Maria Dora Carrion; Carlota Lopez Cara; Olga Cruz-Lopez; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Maria Rosaria Pipitone; Jan Balzarini; Nicola Zonta; Andrea Brancale; Ernest Hamel
Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
Bioorganic & medicinal chemistry 2009;17(19):6862-71.
2009: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Maria Dora Carrion; Olga Cruz-Lopez; Carlota Lopez Cara; Giuseppe Basso; Giampietro Viola; Mohammed Khedr; Jan Balzarini; Siavosh Mahboobi; Andreas Sellmer; Andrea Brancale; Ernest Hamel
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
Journal of medicinal chemistry 2009;52(17):5551-5.
2009: Michael Edler; Guangli Yang; M Katherine Jung; Ruoli Bai; William G Bornmann; Ernest Hamel
Demonstration of microtubule-like structures formed with (-)-rhazinilam from purified tubulin outside of cells and a simple tubulin-based assay for evaluation of analog activity.
Archives of biochemistry and biophysics 2009;487(2):98-104.
2009: Romeo Romagnoli; Pier Giovanni Baraldi; Maria Dora Carrion; Olga Cruz-Lopez; LUISA-CARLOTA LÓPEZ-CARA; Jan Balzarini; Ernest Hamel; Alessandro Canella; Enrica Fabbri; Roberto Gambari; Giuseppe Basso; Giampietro Viola
Hybrid alpha-bromoacryloylamido chalcones. Design, synthesis and biological evaluation.
Bioorganic & medicinal chemistry letters 2009;19(7):2022-8.
2009: Elizabeth Wilcox; Connor McGrath; Andrei V Blokhin; Rick Gussio; Ernest Hamel
Evidence for a distinct ligand binding site on tubulin discovered through inhibition by GDP of paclitaxel-induced tubulin assembly in the absence of exogenous GTP.
Archives of biochemistry and biophysics 2009;484(1):55-62.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Taradas Sarkar; LUISA-CARLOTA LÓPEZ-CARA; Olga Cruz Lopez; Maria Dora Carrion; Delia Preti; Manlio Tolomeo; Jan Balzarini; Ernest Hamel
Synthesis and biological evaluation of 2-aroyl-4-phenyl-5-hydroxybenzofurans as a new class of antitubulin agents.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2008;4(6):558-64.
2008: RAVI ANCHOORI; Madeline Kortenhorst; Manuel Hidalgo; Taradas Sarkar; Gurulingappa Hallur; Ruoli Bai; Paulus van Diest; Ernest Hamel; Saeed R Khan
Novel microtubule-interacting phenoxy pyridine and phenyl sulfanyl pyridine analogues for cancer therapy.
Journal of medicinal chemistry 2008;51(19):5953-7.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Taradas Sarkar; Maria Dora Carrion; Olga Cruz-Lopez; LUISA-CARLOTA LÓPEZ-CARA; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Maria Rosaria Pipitone; Jan Balzarini; Roberto Gambari; Lampronti Ilaria; Roberto Saletti; Andrea Brancale; Ernest Hamel
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
Bioorganic & medicinal chemistry 2008;16(18):8419-26.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Maria Dora Carrion; Olga Cruz-Lopez; LUISA-CARLOTA LÓPEZ-CARA; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Maria Rosa Pipitone; Jan Balzarini; Sahar Kandil; Andrea Brancale; Taradas Sarkar; Ernest Hamel
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
Bioorganic & medicinal chemistry letters 2008;18(18):5041-5.
2008: Shala L Thomas; Diansheng Zhong; Wei Zhou; Sanna Malik; Dennis C Liotta; James P Snyder; Ernest Hamel; Paraskevi Giannakakou
EF24, a novel curcumin analog, disrupts the microtubule cytoskeleton and inhibits HIF-1.
Cell cycle (Georgetown, Tex.) 2008;7(15):2409-17.
2008: Zhenglai Fang; Yunlong Song; Taradas Sarkar; Ernest Hamel; William E Fogler; Gregory E Agoston; Phillip E Fanwick; Mark Cushman
Stereoselective synthesis of 3,3-diarylacrylonitriles as tubulin polymerization inhibitors.
The Journal of organic chemistry 2008;73(11):4241-4.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Olga Cruz-Lopez; Delia Preti; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Nicola Zonta; Jan Balzarini; Andrea Brancale; Taradas Sarkar; Ernest Hamel
Design, synthesis, and biological evaluation of thiophene analogues of chalcones.
Bioorganic & medicinal chemistry 2008;16(10):5367-76.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Taradas Sarkar; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Olga Cruz-Lopez; Delia Preti; Mojgan Aghazadeh Tabrizi; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Nicola Zonta; Jan Balzarini; Andrea Brancale; Hsing-Pang Hsieh; Ernest Hamel
Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
Journal of medicinal chemistry 2008;51(5):1464-8.
2008: Ruoli Bai; Christopher D Vanderwal; J Fernando Díaz; Ernest Hamel
Interaction of a cyclostreptin analogue with the microtubule taxoid site: the covalent reaction rapidly follows binding.
Journal of natural products 2008;71(3):370-4.
2008: Pixu Li; Cory D Evans; Yongzhong Wu; Bin Cao; Ernest Hamel; Madeleine M Joullié
Evolution of the total syntheses of ustiloxin natural products and their analogues.
Journal of the American Chemical Society 2008;130(7):2351-64.
2007: Romeo Romagnoli; Pier Giovanni Baraldi; Vincent Remusat; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Olga Cruz-Lopez; Delia Preti; Francesca Fruttarolo; Mojgan Aghazadeh Tabrizi; Jan Balzarini; Ernest Hamel
Synthesis and biological evaluation of 2-amino-3-(3', 4', 5'-trimethoxy-phenylsulfonyl)-5-aryl thiophenes as a new class of antitubulin agents.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2007;3(6):507-12.
2007: Nima Sharifi; Ernest Hamel; Markus A Lill; Prabhakar Risbood; Charles T Kane; Md Tafazzal Hossain; Amanda Jones; James T Dalton; William L Farrar
A bifunctional colchicinoid that binds to the androgen receptor.
Molecular cancer therapeutics 2007;6(8):2328-36.
2007: Giuseppe La Regina; Michael Edler; Andrea Brancale; Sahar Kandil; Antonio Coluccia; Francesco Piscitelli; Ernest Hamel; Gabriella De Martino; Ruth Matesanz; J Fernando Díaz; Anna Scovassi; Ennio Prosperi; Antonio Lavecchia; Ettore Novellino; Marino Artico; Romano Silvestri
Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.
Journal of medicinal chemistry 2007;50(12):2865-74.
2007: Romeo Romagnoli; Pier Giovanni Baraldi; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Delia Preti; Francesca Fruttarolo; Maria Giovanna Pavani; Mojgan Aghazadeh Tabrizi; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Jan Balzarini; John A Hadfield; Andrea Brancale; Ernest Hamel
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
Journal of medicinal chemistry 2007;50(9):2273-7.
2007: Daniel J Kerr; Ernest Hamel; M Katherine Jung; Bernard L Flynn
The concise synthesis of chalcone, indanone and indenone analogues of combretastatin A4.
Bioorganic & medicinal chemistry 2007;15(9):3290-8.
2007: Rubén M Buey; Enrique Calvo; Isabel Barasoain; Oriol Pineda; Michael Edler; Ruth Matesanz; Gemma Cerezo; Christopher D Vanderwal; Billy W Day; Erik J Sorensen; Juan Antonio López; José Manuel Andreu; Ernest Hamel; J Fernando Díaz
Cyclostreptin binds covalently to microtubule pores and lumenal taxoid binding sites.
Nature chemical biology 2007;3(2):117-25.
2006: Donnette A Dabydeen; James C Burnett; Ruoli Bai; Pascal Verdier-Pinard; Sarah J H Hickford; George R Pettit; John W Blunt; Murray H G Munro; Rick Gussio; Ernest Hamel
Comparison of the activities of the truncated halichondrin B analog NSC 707389 (E7389) with those of the parent compound and a proposed binding site on tubulin.
Molecular pharmacology 2006;70(6):1866-75.
2006: Ernest Hamel; Billy W Day; John H Miller; M Katherine Jung; Peter T Northcote; Arun K Ghosh; Dennis P Curran; Mark Cushman; K C Nicolaou; Ian Paterson; Erik J Sorensen
Synergistic effects of peloruside A and laulimalide with taxoid site drugs, but not with each other, on tubulin assembly.
Molecular pharmacology 2006;70(5):1555-64.
2006: Romeo Romagnoli; Pier Giovanni Baraldi; Vincent Remusat; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Delia Preti; Francesca Fruttarolo; Maria Giovanna Pavani; Mojgan Aghazadeh Tabrizi; Manlio Tolomeo; Stefania Grimaudo; Jan Balzarini; Mary Ann Jordan; Ernest Hamel
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
Journal of medicinal chemistry 2006;49(21):6425-8.
2006: James D White; Helmars Smits; Ernest Hamel
Synthesis of cryptothilone 1, the first cryptophycin-epothilone hybrid.
Organic letters 2006;8(18):3947-50.
2006: Martin G Banwell; Ernest Hamel; David C R Hockless; Pascal Verdier-Pinard; Anthony C Willis; David J Wong
4,5-Diaryl-1H-pyrrole-2-carboxylates as combretastatin A-4/lamellarin T hybrids: synthesis and evaluation as anti-mitotic and cytotoxic agents.
Bioorganic & medicinal chemistry 2006;14(13):4627-38.
2006: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Maria Giovanna Pavani; Mojgan Aghazadeh Tabrizi; Delia Preti; Francesca Fruttarolo; Laura Piccagli; M Katherine Jung; Ernest Hamel; Monica Borgatti; Roberto Gambari
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-5-aryl thiophenes as a new class of potent antitubulin agents.
Journal of medicinal chemistry 2006;49(13):3906-15.
2006: Gabriella De Martino; Michael Edler; Giuseppe La Regina; Antonio Coluccia; Maria Chiara Barbera; Denise Barrow; Robert I Nicholson; Gabriela Chiosis; Andrea Brancale; Ernest Hamel; Marino Artico; Romano Silvestri
New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies.
Journal of medicinal chemistry 2006;49(3):947-54.
2005: Charitha Madiraju; Michael Edler; Ernest Hamel; Brianne S Raccor; Raghavan Balachandran; Guangyu Zhu; Kenneth A Giuliano; Andreas Vogt; Youseung Shin; Jean-Hugues Fournier; Yoshikazu Fukui; Arndt M Brückner; Dennis P Curran; Billy W Day
Tubulin assembly, taxoid site binding, and cellular effects of the microtubule-stabilizing agent dictyostatin.
Biochemistry 2005;44(45):15053-63.
2005: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; M Katherine Jung; Maria Antonietta Iaconinoto; Maria Dora Carrion; Vincent Remusat; Delia Preti; Mojgan Aghazadeh Tabrizi; Fruttarolo Francesca; Erik De Clercq; Jan Balzarini; Ernest Hamel
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
Bioorganic & medicinal chemistry letters 2005;15(18):4048-52.
2005: Michael Edler; Rubén M Buey; Rick Gussio; Marcus Adam; Christopher D Vanderwal; Erik J Sorensen; J Fernando Díaz; Paraskevi Giannakakou; Ernest Hamel
Cyclostreptin (FR182877), an antitumor tubulin-polymerizing agent deficient in enhancing tubulin assembly despite its high affinity for the taxoid site.
Biochemistry 2005;44(34):11525-38.
2005: Youseung Shin; Jean-Hugues Fournier; Raghavan Balachandran; Charitha Madiraju; Brianne S Raccor; Guangyu Zhu; Michael Edler; Ernest Hamel; Billy W Day; Dennis P Curran
Synthesis and biological evaluation of (-)-16-normethyldictyostatin: a potent analogue of (-)-dictyostatin.
Organic letters 2005;7(14):2873-6.
2005: Md Ahad Ali; Robert B Bates; Zackary D Crane; Christopher W Dicus; Michelle R Gramme; Ernest Hamel; Jacob Marcischak; David S Martinez; Kelly J McClure; Pichaya Nakkiew; George R Pettit; Chad C Stessman; Bilal A Sufi; Gayle V Yarick
Dolastatin 11 conformations, analogues and pharmacophore.
Bioorganic & medicinal chemistry 2005;13(13):4138-52.
2005: Marcus Adam; Jun Zhou; Aurora O'Brate; Ernest Hamel; Jason Wong; Michael Nivens; Adel El-Naggar; Tso-Pang Yao; Fadlo R Khuri; Paraskevi Giannakakou
The synergistic combination of the farnesyl transferase inhibitor lonafarnib and paclitaxel enhances tubulin acetylation and requires a functional tubulin deacetylase.
Cancer research 2005;65(9):3883-93.
2005: Daniele Simoni; Giuseppina Grisolia; Giuseppe Giannini; Marinella Roberti; Riccardo Rondanin; Laura Piccagli; Riccardo Baruchello; Marcello Rossi; LUISA-CARLOTA LÓPEZ-CARA; Francesco Paolo Invidiata; Stefania Grimaudo; M Katherine Jung; Ernest Hamel; Nicola Gebbia; Lucia Crosta; Vincenzo Abbadessa; Antonietta Di Cristina; Luisa Dusonchet; Maria Meli; Manlio Tolomeo
Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines.
Journal of medicinal chemistry 2005;48(3):723-36.
2004: Gabriella De Martino; Giuseppe La Regina; Antonio Coluccia; Michael Edler; Maria Chiara Barbera; Andrea Brancale; Elizabeth Wilcox; Ernest Hamel; Marino Artico; Romano Silvestri
Arylthioindoles, potent inhibitors of tubulin polymerization.
Journal of medicinal chemistry 2004;47(25):6120-3.
2004: Ruoli Bai; David G Covell; George F Taylor; John A Kepler; Terry D Copeland; Nga Y Nguyen; George R Pettit; Ernest Hamel
Direct photoaffinity labeling by dolastatin 10 of the amino-terminal peptide of beta-tubulin containing cysteine 12.
The Journal of biological chemistry 2004;279(29):30731-40.
2004: Eric J Gapud; Ruoli Bai; Arun K Ghosh; Ernest Hamel
Laulimalide and paclitaxel: a comparison of their effects on tubulin assembly and their synergistic action when present simultaneously.
Molecular pharmacology 2004;66(1):113-21.
2004: Donnette A Dabydeen; Gordon J Florence; Ian Paterson; Ernest Hamel
A quantitative evaluation of the effects of inhibitors of tubulin assembly on polymerization induced by discodermolide, epothilone B, and paclitaxel.
Cancer chemotherapy and pharmacology 2004;53(5):397-403.
2003: Zobeida Cruz-Monserrate; Jeffrey T Mullaney; Patrick G Harran; George R Pettit; Ernest Hamel
Dolastatin 15 binds in the vinca domain of tubulin as demonstrated by Hummel-Dreyer chromatography.
European journal of biochemistry / FEBS 2003;270(18):3822-8.
2003: Zobeida Cruz-Monserrate; Hélène C Vervoort; Ruoli Bai; David Newman; Stephen B Howell; Gerrit Los; Jeffrey T Mullaney; Michael D Williams; George R Pettit; William Fenical; Ernest Hamel
Diazonamide A and a synthetic structural analog: disruptive effects on mitosis and cellular microtubules and analysis of their interactions with tubulin.
Molecular pharmacology 2003;63(6):1273-80.
2003: Martin G Banwell; Alison J Edwards; Katrina A Jolliffe; Jason A Smith; Ernest Hamel; Pascal Verdier-Pinard
Total synthesis of (+/-)-rhazinal, an alkaloidal spindle toxin from Kopsia teoi.
Organic & biomolecular chemistry 2003;1(2):296-305.
2003: Ernest Hamel
Evaluation of antimitotic agents by quantitative comparisons of their effects on the polymerization of purified tubulin.
Cell biochemistry and biophysics 2003;38(1):1-22.
2002: Ruoli Bai; Robert B Bates; Ernest Hamel; Richard E Moore; Pichaya Nakkiew; George R Pettit; Bilal A Sufi
Lyngbyastatin 1 and Ibu-epilyngbyastatin 1: synthesis, stereochemistry, and NMR line broadening.
Journal of natural products 2002;65(12):1824-9.
2002: Ruoli Bai; David G Covell; Chunfeng Liu; Arun K Ghosh; Ernest Hamel
(-)-Doliculide, a new macrocyclic depsipeptide enhancer of actin assembly.
The Journal of biological chemistry 2002;277(35):32165-71.
2002: Donald E Pryor; Aurora O'Brate; Geoffrey Bilcer; J Fernando Díaz; Yuefang Wang; Yong Wang; Mikio Kabaki; M Katherine Jung; José Manuel Andreu; Arun K Ghosh; Paraskevi Giannakakou; Ernest Hamel
The microtubule stabilizing agent laulimalide does not bind in the taxoid site, kills cells resistant to paclitaxel and epothilones, and may not require its epoxide moiety for activity.
Biochemistry 2002;41(29):9109-15.
2002: Emmanuel A Ojo-Amaize; Emeka J Nchekwube; Howard B Cottam; Ruoli Bai; Pascal Verdier-Pinard; Vellalore N Kakkanaiah; Judith A Varner; Lorenzo Leoni; Joseph I Okogun; Akinbo A Adesomoju; Olusola A Oyemade; Ernest Hamel
Hypoestoxide, a natural nonmutagenic diterpenoid with antiangiogenic and antitumor activity: possible mechanisms of action.
Cancer research 2002;62(14):4007-14.
2002: Bernard L Flynn; Ernest Hamel; M Katherine Jung
One-pot synthesis of benzo[b]furan and indole inhibitors of tubulin polymerization.
Journal of medicinal chemistry 2002;45(12):2670-3.
2002: Brian L Marquez; Karl Shawn Watts; Alexandre F T Yokochi; Mary Ann Roberts; Pascal Verdier-Pinard; Jorge I Jimenez; Ernest Hamel; Paul J Scheuer; William H Gerwick
Structure and absolute stereochemistry of hectochlorin, a potent stimulator of actin assembly.
Journal of natural products 2002;65(6):866-71.
2002: Ernest Hamel; David G Covell
Antimitotic peptides and depsipeptides.
Current medicinal chemistry. Anti-cancer agents 2002;2(1):19-53.
2002: Ernest Hamel
Interactions of antimitotic peptides and depsipeptides with tubulin.
Biopolymers 2002;66(3):142-60.
2001: Bernard L Flynn; G P Flynn; Ernest Hamel; M Katherine Jung
The synthesis and tubulin binding activity of thiophene-based analogues of combretastatin A-4.
Bioorganic & medicinal chemistry letters 2001;11(17):2341-3.
2001: Bernard L Flynn; Pascal Verdier-Pinard; Ernest Hamel
A novel palladium-mediated coupling approach to 2,3-disubstituted benzo(b)thiophenes and its application to the synthesis of tubulin binding agents.
Organic letters 2001;3(5):651-4.
2001: Ruoli Bai; Pascal Verdier-Pinard; S Gangwar; Chad C Stessman; K J McClure; Edward A Sausville; George R Pettit; Robert B Bates; Ernest Hamel
Dolastatin 11, a marine depsipeptide, arrests cells at cytokinesis and induces hyperpolymerization of purified actin.
Molecular pharmacology 2001;59(3):462-9.
2000: Ruoli Bai; David G Covell; X F Pei; JB Ewell; Nga Y Nguyen; Arnold Brossi; Ernest Hamel
Mapping the binding site of colchicinoids on beta -tubulin. 2-Chloroacetyl-2-demethylthiocolchicine covalently reacts predominantly with cysteine 239 and secondarily with cysteine 354.
The Journal of biological chemistry 2000;275(51):40443-52.
2000: Lorenzo Leoni; Ernest Hamel; Davide Genini; Hsiencheng Shih; CJ Carrera; Howard B Cottam; Dennis A Carson
Indanocine, a microtubule-binding indanone and a selective inducer of apoptosis in multidrug-resistant cancer cells.
Journal of the National Cancer Institute 2000;92(3):217-24.
1999: Ruoli Bai; N A Durso; D L Sackett; Ernest Hamel
Interactions of the sponge-derived antimitotic tripeptide hemiasterlin with tubulin: comparison with dolastatin 10 and cryptophycin 1.
Biochemistry 1999;38(43):14302-10.
1999: Pascal Verdier-Pinard; Namthip Sitachitta; J V Rossi; D L Sackett; William H Gerwick; Ernest Hamel
Biosynthesis of radiolabeled curacin A and its rapid and apparently irreversible binding to the colchicine site of tubulin.
Archives of biochemistry and biophysics 1999;370(1):51-8.
1999: William R Gamble; N A Durso; RW Fuller; CK Westergaard; Tanya R Johnson; D L Sackett; Ernest Hamel; John H Cardellina; Michael R Boyd
Cytotoxic and tubulin-interactive hemiasterlins from Auletta sp. and Siphonochalina spp. sponges.
Bioorganic & medicinal chemistry 1999;7(8):1611-5.
1999: Ruoli Bai; JB Ewell; Nga Y Nguyen; Ernest Hamel
Direct photoaffinity labeling of cysteine 211 or a nearby amino acid residue of beta-tubulin by guanosine 5'-diphosphate bound in the exchangeable site.
The Journal of biological chemistry 1999;274(18):12710-4.
1999: Ernest Hamel; D L Sackett; D Vourloumis; K C Nicolaou
The coral-derived natural products eleutherobin and sarcodictyins A and B: effects on the assembly of purified tubulin with and without microtubule-associated proteins and binding at the polymer taxoid site.
Biochemistry 1999;38(17):5490-8.
1998: Brian L Márquez; Pascal Verdier-Pinard; Ernest Hamel; William H Gerwick
Curacin D, an antimitotic agent from the marine cyanobacterium Lyngbya majuscula.
Phytochemistry 1998;49(8):2387-9.
1998: John A Beutler; Ernest Hamel; A J Vlietinck; Achiel Haemers; P Rajan; J N Roitman; John H Cardellina; Michael R Boyd
Structure-activity requirements for flavone cytotoxicity and binding to tubulin.
Journal of medicinal chemistry 1998;41(13):2333-8.
1998: Ruoli Bai; K Choe; JB Ewell; Nga Y Nguyen; Ernest Hamel
Direct photoaffinity labeling of cysteine-295 of alpha-tubulin by guanosine 5'-triphosphate bound in the nonexchangeable site.
The Journal of biological chemistry 1998;273(16):9894-7.
1998: Pascal Verdier-Pinard; J Y Lai; Hye-Dong Yoo; J Yu; Brian L Marquez; D G Nagle; M Nambu; J D White; J R Falck; William H Gerwick; B W Day; Ernest Hamel
Structure-activity analysis of the interaction of curacin A, the potent colchicine site antimitotic agent, with tubulin and effects of analogs on the growth of MCF-7 breast cancer cells.
Molecular pharmacology 1998;53(1):62-76.
1997: Richard Kowalski; P Giannakakou; Sarath P Gunasekera; Ross E Longley; B W Day; Ernest Hamel
The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and inhibits the growth of paclitaxel-resistant cells.
Molecular pharmacology 1997;52(4):613-22.
1997: E ter Haar; Ernest Hamel; Raghavan Balachandran; Billy W Day
Cellular targets of the anti-breast cancer agent Z-1,1-dichloro-2,3-diphenylcyclopropane: type II estrogen binding sites and tubulin.
Anticancer research 1997;17(3C):1861-9.
1997: S S Jonnalagadda; E ter Haar; Ernest Hamel; C M Lin; R A Magarian; Billy W Day
Synthesis and biological evaluation of 1,1-dichloro-2,3-diarylcyclopropanes as antitubulin and anti-breast cancer agents.
Bioorganic & medicinal chemistry 1997;5(4):715-22.
1997: Richard Kowalski; P Giannakakou; Ernest Hamel
Activities of the microtubule-stabilizing agents epothilones A and B with purified tubulin and in cells resistant to paclitaxel (Taxol(R)).
The Journal of biological chemistry 1997;272(4):2534-41.