Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents
Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents
复制标题
新型二氢芳基/烷基硫基-环己基甲基-氧代嘧啶（S-DACO）作为高活性抗HIV药物的合成和生物学评价
DOI：
10.1016/j.bmcl.2010.12.003
复制
发表时间：
2011-01-15
影响因子：
2.7
通讯作者：
Zheng, Yong-Tang
中科院分区：
文献类型：
--
作者：
He, Yan-Ping;Long, Jin;Zheng, Yong-Tang
以奈韦拉平（Nevirapine，NVP）和齐多夫定（Zidovudine，AZT）为阳性对照，合成了一种新型的二氢芳基/烷硫基环己基甲基氧代嘧啶（dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines，S-DACOs）组合库，并在体外对HIV-1（IIIB）感染的C8166细胞进行了评价。抗HIV筛选结果表明，C-6-环己基甲基取代的嘧啶酮比6-芳甲基取代的嘧啶酮具有更高的选择性指数。化合物1g、1c、1 e和1b显示出有效的抗HIV活性，其EC 50值分别为0.012、0.025、0.088和0.162 nM。(C)2010爱思唯尔有限公司保留所有权利。
A novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) combinatory library was synthesized and evaluated with C8166 cells infected by the HIV-1(IIIB) in vitro, using Nevirapine (NVP) and Zidovudine (AZT) as positive control. The anti-HIV screening results revealed that C-6-cyclohexylmethyl substituted pyrimidinones possessed higher selective index than its 6-arylmethyl counterparts. Compounds 1g, 1c, 1e and 1b showed potent anti-HIV activities with EC50 values of 0.012, 0.025, 0.088 and 0.162 nM, respectively. (C) 2010 Elsevier Ltd. All rights reserved.