在烯基二芳基甲烷（ADAM）系列中合成具有优化效力和治疗指数的非核苷类逆转录酶抑制剂。
Synthesis of a non-nucleoside reverse transcriptase inhibitor in the alkenyldiarylmethane (ADAM) series with optimized potency and therapeutic index.
作者信息
Cushman M, Casimiro-Garcia A, Williamson K, Rice W G
机构信息
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907, USA.
出版信息
Bioorg Med Chem Lett. 1998 Jan 20;8(2):195-8. doi: 10.1016/s0960-894x(97)10214-1.
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-1RF in CEM-SS cells with an EC50 of 13 nM, while it shows cytotoxicity with a CC50 of 31.6 microM, providing a therapeutic index of 2430. ADAM II is a non-nucleoside reverse transcriptase inhibitor, displaying an IC50 of 0.3 microM with poly(rC) oligo(dG) as the template/primer.
一种新型的烯基二芳基甲烷（ADAM）类似物已被合成出来，作为一种抗HIV药物，其效力有所增强。这种新化合物（ADAM II）在CEM-SS细胞中抑制HIV-1RF的细胞病变效应，半数有效浓度（EC50）为13 nM，而其细胞毒性的半数致死浓度（CC50）为31.6 μM，治疗指数为2430。ADAM II是一种非核苷类逆转录酶抑制剂，以聚（rC）寡聚（dG）作为模板/引物时，其半数抑制浓度（IC50）为0.3 μM。
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