| Literature DB >> 18451566 |
Hui Xu1, Wu-Qing Liu, Ling-Ling Fan, Yang Chen, Liu-Meng Yang, Lei Lv, Yong-Tang Zheng.
Abstract
Eight simple N-arylindoles were designed, synthesized and evaluated as human immunodeficiency virus (HIV)-1 integrase inhibitors in vitro for the first time. Among these compounds, 3b, 3e and 3g demonstrated significant anti-HIV-1 integrase activity. Especially 3b showed the highest anti-HIV-1 integrase activity with EC50 value of 7.88 microg/ml and TI value of 24.61. Meantime, some structure-activity relationships were also observed and will provide a new lead for design and discovery of more potent N-arylindoles as HIV-1 integrase inhibitors.Entities:
Mesh：
Substances：
Year: 2008 PMID： 18451566 DOI： 10.1248/cpb.56.720
Source DB: PubMed Journal: Chem Pharm Bull (Tokyo) ISSN： 0009-2363 Impact factor: 1.645