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Ion Niculescu-Duvaz

Research Profile

Chemicals & Drugs

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Anatomy

Genes & Molecular Sequences

Transgenic Suicide Genes

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Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Jean-Francois Pons; Lawrence Davies; Richard Marais; Delphine Ménard; Bart M J M Suijkerbuijk; Steven Whittaker; Alfonso Zambon; Caroline J Springer
Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents.
Alfonso Zambon; Richard Marais; Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Caroline J Springer
BRAF as a therapeutic target: a patent review (2006 - 2012).
Leisl M Packer; Sareena Rana; Ana Rebocho; Caroline Springer; Matthew S Zabriskie; Brian J Druker; Christopher A Eide; Robert Hayward; Sonja Heidorn; Ion Niculescu-Duvaz; Thomas O'Hare; Richard Marais
Nilotinib and MEK inhibitors induce synthetic lethality through paradoxical activation of RAF in drug-resistant chronic myeloid leukemia.

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All Publications

2013: Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Jean-Francois Pons; Lawrence Davies; Richard Marais; Delphine Ménard; Bart M J M Suijkerbuijk; Steven Whittaker; Alfonso Zambon; Caroline J Springer
Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents.
Bioorganic & medicinal chemistry 2013;21(5):1284-304.
2013: Alfonso Zambon; Richard Marais; Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Caroline J Springer
BRAF as a therapeutic target: a patent review (2006 - 2012).
Expert opinion on therapeutic patents 2013;23(2):155-64.
2011: Leisl M Packer; Sareena Rana; Ana Rebocho; Caroline Springer; Matthew S Zabriskie; Brian J Druker; Christopher A Eide; Robert Hayward; Sonja Heidorn; Ion Niculescu-Duvaz; Thomas O'Hare; Richard Marais
Nilotinib and MEK inhibitors induce synthetic lethality through paradoxical activation of RAF in drug-resistant chronic myeloid leukemia.
Cancer cell 2011;20(6):715-27.
2010: Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Bart M J M Suijkerbuijk; Delphine Ménard; Alfonso Zambon; Arnaud Nourry; Lawrence Davies; Helen Anuradha Manne; Frank Friedlos; Lesley M Ogilvie; Douglas Hedley; Andrew K Takle; David M Wilson; Jean-Francois Pons; Tom Coulter; Ruth Kirk; Neus Cantarino; Steven Whittaker; Richard Marais; Caroline J Springer
Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.
Bioorganic & medicinal chemistry 2010;18(18):6934-52.
2010: Alfonso Zambon; Delphine Ménard; Bart M J M Suijkerbuijk; Ion Niculescu-Duvaz; Steven Whittaker; Dan Niculescu-Duvaz; Arnaud Nourry; Lawrence Davies; Helen Anuradha Manne; Filipa Lopes; Natasha Preece; Douglas Hedley; Lesley M Ogilvie; Ruth Kirk; Richard Marais; Caroline J Springer
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.
Journal of medicinal chemistry 2010;53(15):5639-55.
2010: Ion Niculescu-Duvaz
Trastuzumab emtansine, an antibody-drug conjugate for the treatment of HER2+ metastatic breast cancer.
Current opinion in molecular therapeutics 2010;12(3):350-60.
2010: Bart M J M Suijkerbuijk; Ion Niculescu-Duvaz; Catherine Gaulon; Harmen P Dijkstra; Dan Niculescu-Duvaz; Delphine Ménard; Alfonso Zambon; Arnaud Nourry; Lawrence Davies; Helen Anuradha Manne; Frank Friedlos; Lesley M Ogilvie; Douglas Hedley; Filipa Lopes; Natasha P U Preece; Javier Moreno-Farre; Florence I Raynaud; Ruth Kirk; Steven Whittaker; Richard Marais; Caroline J Springer
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.
Journal of medicinal chemistry 2010;53(7):2741-56.
2010: Arnaud Nourry; Alfonso Zambon; Lawrence Davies; Ion Niculescu-Duvaz; Harmen P Dijkstra; Delphine Ménard; Catherine Gaulon; Dan Niculescu-Duvaz; Bart M J M Suijkerbuijk; Frank Friedlos; Helen Anuradha Manne; Ruth Kirk; Steven Whittaker; Richard Marais; Caroline J Springer
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.
Journal of medicinal chemistry 2010;53(5):1964-78.
2009: Delphine Ménard; Ion Niculescu-Duvaz; Harmen P Dijkstra; Dan Niculescu-Duvaz; Bart M J M Suijkerbuijk; Alfonso Zambon; Arnaud Nourry; Esteban Roman; Lawrence Davies; Helen Anuradha Manne; Frank Friedlos; Ruth Kirk; Steven Whittaker; Adrian Gill; Richard Taylor; Richard Marais; Caroline J Springer
Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.
Journal of medicinal chemistry 2009;52(13):3881-91.
2009: Dan Niculescu-Duvaz; Catherine Gaulon; Harmen P Dijkstra; Ion Niculescu-Duvaz; Alfonso Zambon; Delphine Ménard; Bart M J M Suijkerbuijk; Arnaud Nourry; Lawrence Davies; Helen Anuradha Manne; Frank Friedlos; Lesley M Ogilvie; Douglas Hedley; Steven Whittaker; Ruth Kirk; Adrian Gill; Richard Taylor; Florence I Raynaud; Javier Moreno-Farre; Richard Marais; Caroline J Springer
Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).
Journal of medicinal chemistry 2009;52(8):2255-64.
2008: Ion Niculescu-Duvaz; Esteban Roman; Steven R Whittaker; Frank Friedlos; Ruth Kirk; Ian J Scanlon; Lawrence C Davies; Dan Niculescu-Duvaz; Richard Marais; Caroline J Springer
Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold.
Journal of medicinal chemistry 2008;51(11):3261-74.
2006: Ion Niculescu-Duvaz; Esteban Roman; Steven R Whittaker; Frank Friedlos; Ruth Kirk; Ian Scanlon; Lawrence C Davies; Dan Niculescu-Duvaz; Richard Marais; Caroline J Springer
Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.
Journal of medicinal chemistry 2006;49(1):407-16.
2005: Ion Niculescu-Duvaz; Caroline J Springer
Introduction to the background, principles, and state of the art in suicide gene therapy.
Molecular biotechnology 2005;30(1):71-88.
2004: Ion Niculescu-Duvaz
Technology evaluation: EMD-273063, EMD Lexigen.
Current opinion in molecular therapeutics 2004;6(5):559-66.
2004: Ion Niculescu-Duvaz; Ian Scanlon; Dan Niculescu-Duvaz; Frank Friedlos; Janet Martin; Richard Marais; Caroline J Springer
Significant differences in biological parameters between prodrugs cleavable by carboxypeptidase G2 that generate 3,5-difluoro-phenol and -aniline nitrogen mustards in gene-directed enzyme prodrug therapy systems.
Journal of medicinal chemistry 2004;47(10):2651-8.
2004: Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Caroline J Springer
Design of prodrugs for suicide gene therapy.
Methods in molecular medicine 2004;90():161-202.
2004: Ion Niculescu-Duvaz; Caroline J Springer
Introduction to the background, principles, and state of the art in suicide gene therapy.
Methods in molecular medicine 2004;90():1-27.
2003: Ian Scanlon; Panos Lehouritis; Ion Niculescu-Duvaz; Richard Marais; Caroline J Springer
Gene regulation in cancer gene therapy strategies.
Current medicinal chemistry 2003;10(20):2175-84.
2003: Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Frank Friedlos; Jan Martin; Panos Lehouritis; Richard Marais; Caroline J Springer
Self-immolative nitrogen mustards prodrugs cleavable by carboxypeptidase G2 (CPG2) showing large cytotoxicity differentials in GDEPT.
Journal of medicinal chemistry 2003;46(9):1690-705.
2002: Ion Niculescu-Duvaz
Glufosfamide (Baxter Oncology).
Current opinion in investigational drugs (London, England : 2000) 2002;3(10):1527-32.
2002: Frank Friedlos; Lawrence Davies; Ian Scanlon; Lesley M Ogilvie; Janet Martin; Stephen M Stribbling; Robert Spooner; Ion Niculescu-Duvaz; Richard Marais; Caroline J Springer
Three new prodrugs for suicide gene therapy using carboxypeptidase G2 elicit bystander efficacy in two xenograft models.
Cancer research 2002;62(6):1724-9.
2002: David H Kirn; Ion Niculescu-Duvaz; Gunnel Hallden; Caroline J Springer
The emerging fields of suicide gene therapy and virotherapy.
Trends in molecular medicine 2002;8(4 Suppl):S68-73.
2000: Ion Niculescu-Duvaz
Technology evaluation: gemtuzumab ozogamicin, Celltech Group.
Current opinion in molecular therapeutics 2000;2(6):691-6.
2000: Caroline J Springer; Ion Niculescu-Duvaz
Prodrug-activating systems in suicide gene therapy.
The Journal of clinical investigation 2000;105(9):1161-7.
2000: Caroline J Springer; Ion Niculescu-Duvaz
Approaches to gene-directed enzyme prodrug therapy (GDEPT).
Advances in experimental medicine and biology 2000;465():403-9.
1999: Ion Niculescu-Duvaz; Frank Friedlos; Dan Niculescu-Duvaz; Lawrence Davies; Caroline J Springer
Prodrugs for antibody- and gene-directed enzyme prodrug therapies (ADEPT and GDEPT).
Anti-cancer drug design 1999;14(6):517-38.
1999: Ion Niculescu-Duvaz; R G Cooper; Stephen M Stribbling; James A Heyes; J A Metcalfe; Caroline J Springer
Recent developments in gene-directed enzyme prodrug therapy (GDEPT) for cancer.
Current opinion in molecular therapeutics 1999;1(4):480-6.
1999: Ion Niculescu-Duvaz; Dan Niculescu-Duvaz; Frank Friedlos; Robert Spooner; Janet Martin; Richard Marais; Caroline J Springer
Self-immolative anthracycline prodrugs for suicide gene therapy.
Journal of medicinal chemistry 1999;42(13):2485-9.
1998: Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Frank Friedlos; Janet Martin; Robert Spooner; Lawrence Davies; Richard Marais; Caroline J Springer
Self-immolative nitrogen mustard prodrugs for suicide gene therapy.
Journal of medicinal chemistry 1998;41(26):5297-309.
1998: Ion Niculescu-Duvaz; Robert Spooner; Richard Marais; Caroline J Springer
Gene-directed enzyme prodrug therapy.
Bioconjugate chemistry 1998;9(1):4-22.
1997: Ion Niculescu-Duvaz; Caroline J Springer
Gene-directed enzyme prodrug therapy: a review of enzyme/prodrug combinations.
Expert opinion on investigational drugs 1997;6(6):685-703.
1996: D C Blakey; P J Burke; D H Davies; R I Dowell; S J East; K P Eckersley; J E Fitton; J McDaid; R G Melton; Ion Niculescu-Duvaz; P E Pinder; S K Sharma; A F Wright; Caroline J Springer
ZD2767, an improved system for antibody-directed enzyme prodrug therapy that results in tumor regressions in colorectal tumor xenografts.
Cancer research 1996;56(14):3287-92.
1995: Caroline J Springer; R Dowell; P J Burke; E Hadley; D H Davis; D C Blakey; R G Melton; Ion Niculescu-Duvaz
Optimization of alkylating agent prodrugs derived from phenol and aniline mustards: a new clinical candidate prodrug (ZD2767) for antibody-directed enzyme prodrug therapy (ADEPT).
Journal of medicinal chemistry 1995;38(26):5051-65.
1995: Caroline J Springer; Ion Niculescu-Duvaz
Antibody-directed enzyme prodrug therapy (ADEPT) with mustard prodrugs.
Anti-cancer drug design 1995;10(5):361-72.
1994: Caroline J Springer; Ion Niculescu-Duvaz; R Barbara Pedley
Novel prodrugs of alkylating agents derived from 2-fluoro- and 3-fluorobenzoic acids for antibody-directed enzyme prodrug therapy.
Journal of medicinal chemistry 1994;37(15):2361-70.