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Michael Kukla

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Chemicals & Drugs

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Physiology

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Publications

TOP 3
Ashis K Saha; Li Liu; Richard Simoneaux; Bart DeCorte; Christophe Meyer; Stacy Skrzat; Henry J Breslin; Michael J Kukla; David W End
Novel triazole based inhibitors of Ras farnesyl transferase.
Paul A J Janssen; Paul J Lewi; Eddy Arnold; Frits Daeyaert; Marc de Jonge; Jan Heeres; Lucien M H Koymans; Maarten Vinkers; Jérôme Guillemont; Elisabeth Pasquier; Michael J Kukla; Donald W Ludovici; Koen Andries; Marie-Pierre de Bethune; Rudi Pauwels; Kalyan Das; Arthur D Clark; Yulia Volovik Frenkel; Stephen H Hughes; Bart Medaer; Fons De Knaep; Hilde Bohets; Fred De Clerck; Ann Lampo; Peter Williams; Paul Stoffels
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
Koen Andries; Hilde Azijn; Theo Thielemans; Donald W Ludovici; Michael J Kukla; Jan Heeres; Paul Janssen; Bart De Corte; Johan Vingerhoets; Rudi Pauwels; Marie-Pierre de Bethune
TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1.

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All Publications

2005: Ashis K Saha; Li Liu; Richard Simoneaux; Bart DeCorte; Christophe Meyer; Stacy Skrzat; Henry J Breslin; Michael J Kukla; David W End
Novel triazole based inhibitors of Ras farnesyl transferase.
Bioorganic & medicinal chemistry letters 2005;15(24):5407-11.
2005: Paul A J Janssen; Paul J Lewi; Eddy Arnold; Frits Daeyaert; Marc de Jonge; Jan Heeres; Lucien M H Koymans; Maarten Vinkers; Jérôme Guillemont; Elisabeth Pasquier; Michael J Kukla; Donald W Ludovici; Koen Andries; Marie-Pierre de Bethune; Rudi Pauwels; Kalyan Das; Arthur D Clark; Yulia Volovik Frenkel; Stephen H Hughes; Bart Medaer; Fons De Knaep; Hilde Bohets; Fred De Clerck; Ann Lampo; Peter Williams; Paul Stoffels
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
Journal of medicinal chemistry 2005;48(6):1901-9.
2004: Koen Andries; Hilde Azijn; Theo Thielemans; Donald W Ludovici; Michael J Kukla; Jan Heeres; Paul Janssen; Bart De Corte; Johan Vingerhoets; Rudi Pauwels; Marie-Pierre de Bethune
TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1.
Antimicrobial agents and chemotherapy 2004;48(12):4680-6.
2004: Kalyan Das; Arthur D Clark; Paul J Lewi; Jan Heeres; Marc R. de Jonge; Lucien M H Koymans; H Maarten Vinkers; Frits Daeyaert; Donald W Ludovici; Michael J Kukla; Bart De Corte; Robert W Kavash; Chih Y Ho; Hong Ye; Mark A Lichtenstein; Koen Andries; Rudi Pauwels; Marie-Pierre de Bethune; Paul L Boyer; Patrick Clark; Stephen H Hughes; Paul A J Janssen; Eddy Arnold
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants.
Journal of medicinal chemistry 2004;47(10):2550-60.
2003: Henry J Breslin; Tamara A Miskowski; Michael J Kukla; Hans L De Winter; Maria V F Somers; Peter W M Roevens; Robert W Kavash
Tripeptidyl-peptidase II (TPP II) inhibitory activity of (S)-2,3-dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a systematic SAR evaluation. Part 2.
Bioorganic & medicinal chemistry letters 2003;13(24):4467-71.
2003: Paul J Lewi; Marc de Jonge; Frits Daeyaert; Lucien M H Koymans; Maarten Vinkers; Jan Heeres; Paul A J Janssen; Eddy Arnold; Kalyan Das; Arthur D Clark; Stephen H Hughes; Paul L Boyer; Marie-Pierre de Bethune; Rudi Pauwels; Koen Andries; Michael J Kukla; Donald W Ludovici; Bart De Corte; Robert W Kavash; Chih Ho; Paul J Lewis
On the detection of multiple-binding modes of ligands to proteins, from biological, structural, and modeling data.
Journal of computer-aided molecular design 2003;17(2-4):129-34.
2002: Henry J Breslin; Tamara A Miskowski; Michael J Kukla; William H Leister; Hans L De Winter; Diane A Gauthier; Maria V F Somers; Daniëlle C G Peeters; Peter W M Roevens
Design, synthesis, and tripeptidyl peptidase II inhibitory activity of a novel series of (S)-2,3-dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles.
Journal of medicinal chemistry 2002;45(24):5303-10.
2001: Donald W Ludovici; Bart De Corte; Michael J Kukla; Hong Ye; Chih Y Ho; M A Lichtenstein; Robert W Kavash; Koen Andries; Marie-Pierre de Bethune; Hilde Azijn; Rudi Pauwels; Paul J Lewi; Jan Heeres; Lucien M H Koymans; Marc R. de Jonge; Koen J A Van Aken; Frits Daeyaert; Kalyan Das; Eddy Arnold; Paul A J Janssen
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
Bioorganic & medicinal chemistry letters 2001;11(17):2235-9.
2001: Donald W Ludovici; Robert W Kavash; Michael J Kukla; Chih Y Ho; Hong Ye; Bart De Corte; Koen Andries; Marie-Pierre de Bethune; Hilde Azijn; Rudi Pauwels; HE Moereels; Jan Heeres; Lucien M H Koymans; Marc R. de Jonge; Koen J A Van Aken; Frits Daeyaert; Paul J Lewi; Kalyan Das; Eddy Arnold; Paul A J Janssen
Evolution of anti-HIV drug candidates. Part 2: Diaryltriazine (DATA) analogues.
Bioorganic & medicinal chemistry letters 2001;11(17):2229-34.
2001: Donald W Ludovici; Michael J Kukla; P G Grous; S Krishnan; Koen Andries; Marie-Pierre de Bethune; Hilde Azijn; Rudi Pauwels; E De Clercq; Eddy Arnold; Paul A J Janssen
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
Bioorganic & medicinal chemistry letters 2001;11(17):2225-8.
2000: Ashis K Saha; Li Liu; Richard Simoneaux; Michael J Kukla; Patrick Marichal; Frank C Odds
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
Bioorganic & medicinal chemistry letters 2000;10(19):2175-8.
1999: Henry J Breslin; Michael J Kukla; T Kromis; H Cullis; F De Knaep; Rudi Pauwels; Koen Andries; E De Clercq; M A Janssen; Paul A J Janssen
Synthesis and anti-HIV activity of 1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one (TBO) derivatives. Truncated 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2( 1H)-on es (TIBO) analogues.
Bioorganic & medicinal chemistry 1999;7(11):2427-36.