Synthesis of a non-nucleoside reverse transcriptase inhibitor in the alkenyldiarylmethane (ADAM) series with optimized potency and therapeutic index

被引：23

作者：

Cushman, M ^{[1
]}

Casimiro-Garcia, A

Williamson, K

Rice, WG

机构：

[1] Purdue Univ, Sch Pharm & Pharmacal Sci, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA

[2] NCI, Lab Antiviral Drug Mechanisms, SAIC Frederick, Frederick Canc Res & Dev Ctr, Frederick, MD 21702 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(97)10214-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel alkenyldiarylmethane (ADAM) analog has been synthesized with enhanced potency as an anti-HIV agent. The new compound (ADAM II) inhibits the cytopathic effect of HIV-1(RF) in CEM-SS cells with an EC50 of 13 nM, while it shows cytotoxicity with a CC50 of 31.6 mu M, providing a therapeutic index of 2430. ADAM II is a non-nucleoside reverse transcriptase inhibitor, displaying an IC50 of 0.3 mu M with poly(rC) oligo(dG) as the template/primer. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：195 / 198

页数：4

共 21 条

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