State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Chem Biol Drug Des. 2013 Jun;81(6):730-41. doi: 10.1111/cbdd.12119.
Compound 1 (VEC-5) was identified as a potent small-molecular HIV-1 viron infectivity factor inhibitor that targets the viron infectivity factor-ElonginC interaction. A structure-activity relationship study was carried out to develop compounds with improved efficacy against HIV-1 and 49 indolizine derivatives of three categories were designed and synthesized. We found that five compounds exhibited promising anti-HIV-1 activity, and the most active compound 2g had an IC50 value of 11.0 μm. These results provide new information to develop highly potent small-molecule HIV-1 viron infectivity factor inhibitors.
化合物 1（VEC-5）被鉴定为一种有效的 HIV-1 病毒感染力因子抑制剂，其作用靶点为病毒感染力因子-ElonginC 相互作用。为了开发针对 HIV-1 的疗效更好的化合物，进行了构效关系研究，并设计和合成了三类 49 个吲唑衍生物。我们发现，有 5 个化合物表现出有前景的抗 HIV-1 活性，其中最活性化合物 2g 的 IC50 值为 11.0 μm。这些结果为开发高效的小分子 HIV-1 病毒感染力因子抑制剂提供了新的信息。
