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Page 1
Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H.
Chung S, Himmel DM, Jiang JK, Wojtak K, Bauman JD, Rausch JW, Wilson JA, Beutler JA, Thomas CJ, Arnold E, Le Grice SF. Chung S, et al. Among authors: arnold e. J Med Chem. 2011 Jul 14;54(13):4462-73. doi: 10.1021/jm2000757. Epub 2011 Jun 2. J Med Chem. 2011. PMID: 21568335 Free PMC article.
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.
Das K, Clark AD Jr, Lewi PJ, Heeres J, De Jonge MR, Koymans LM, Vinkers HM, Daeyaert F, Ludovici DW, Kukla MJ, De Corte B, Kavash RW, Ho CY, Ye H, Lichtenstein MA, Andries K, Pauwels R, De Béthune MP, Boyer PL, Clark P, Hughes SH, Janssen PA, Arnold E. Das K, et al. Among authors: arnold e. J Med Chem. 2004 May 6;47(10):2550-60. doi: 10.1021/jm030558s. J Med Chem. 2004. PMID: 15115397
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).
Janssen PA, Lewi PJ, Arnold E, Daeyaert F, de Jonge M, Heeres J, Koymans L, Vinkers M, Guillemont J, Pasquier E, Kukla M, Ludovici D, Andries K, de Béthune MP, Pauwels R, Das K, Clark AD Jr, Frenkel YV, Hughes SH, Medaer B, De Knaep F, Bohets H, De Clerck F, Lampo A, Williams P, Stoffels P. Janssen PA, et al. Among authors: arnold e. J Med Chem. 2005 Mar 24;48(6):1901-9. doi: 10.1021/jm040840e. J Med Chem. 2005. PMID: 15771434 Review.
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
Heeres J, de Jonge MR, Koymans LM, Daeyaert FF, Vinkers M, Van Aken KJ, Arnold E, Das K, Kilonda A, Hoornaert GJ, Compernolle F, Cegla M, Azzam RA, Andries K, de Béthune MP, Azijn H, Pauwels R, Lewi PJ, Janssen PA. Heeres J, et al. Among authors: arnold e. J Med Chem. 2005 Mar 24;48(6):1910-8. doi: 10.1021/jm040829e. J Med Chem. 2005. PMID: 15771435
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
Benjahad A, Croisy M, Monneret C, Bisagni E, Mabire D, Coupa S, Poncelet A, Csoka I, Guillemont J, Meyer C, Andries K, Pauwels R, de Béthune MP, Himmel DM, Das K, Arnold E, Nguyen CH, Grierson DS. Benjahad A, et al. Among authors: arnold e. J Med Chem. 2005 Mar 24;48(6):1948-64. doi: 10.1021/jm0408621. J Med Chem. 2005. PMID: 15771439
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
Guillemont J, Pasquier E, Palandjian P, Vernier D, Gaurrand S, Lewi PJ, Heeres J, de Jonge MR, Koymans LM, Daeyaert FF, Vinkers MH, Arnold E, Das K, Pauwels R, Andries K, de Béthune MP, Bettens E, Hertogs K, Wigerinck P, Timmerman P, Janssen PA. Guillemont J, et al. Among authors: arnold e. J Med Chem. 2005 Mar 24;48(6):2072-9. doi: 10.1021/jm040838n. J Med Chem. 2005. PMID: 15771449
Crystal structures for HIV-1 reverse transcriptase in complexes with three pyridinone derivatives: a new class of non-nucleoside inhibitors effective against a broad range of drug-resistant strains.
Himmel DM, Das K, Clark AD Jr, Hughes SH, Benjahad A, Oumouch S, Guillemont J, Coupa S, Poncelet A, Csoka I, Meyer C, Andries K, Nguyen CH, Grierson DS, Arnold E. Himmel DM, et al. Among authors: arnold e. J Med Chem. 2005 Dec 1;48(24):7582-91. doi: 10.1021/jm0500323. J Med Chem. 2005. PMID: 16302798
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.
Himmel DM, Sarafianos SG, Dharmasena S, Hossain MM, McCoy-Simandle K, Ilina T, Clark AD Jr, Knight JL, Julias JG, Clark PK, Krogh-Jespersen K, Levy RM, Hughes SH, Parniak MA, Arnold E. Himmel DM, et al. Among authors: arnold e. ACS Chem Biol. 2006 Dec 20;1(11):702-12. doi: 10.1021/cb600303y. ACS Chem Biol. 2006. PMID: 17184135 Free PMC article.
955 results