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Synthesis and Biological Evaluation of (±)-benzhydrol Derivatives as Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

Synthesis and Biological Evaluation of (±)-benzhydrol Derivatives as Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

Xiao-Dong Ma, Xuan Zhang, Shi-Qiong Yang, Hui-Fang Dai, Liu-Meng Yang, Shuang-Xi Gu, Yong-Tang Zheng, Qiu-Qin He, Fen-Er Chen

Bioorg Med Chem. 2011 Aug 15;19(16):4704-9.

PMID: 21788138

Abstract:

A series of (±)-benzhydrol derivatives featuring the essential sulfonamide group at the para position on the C-ring were synthesized and evaluated for the potential anti-HIV activity in C8166 cells. Most of these analogues demonstrated low concentration inhibitory activity with EC(50) values less than 1 μM against the wild-type HIV-1. In particular, compound 7h was identified as the highest active inhibitor of wild-type HIV-1 with an EC(50) value of 0.12 μM and selectivity index value of 312.73. Furthermore, some of them also exhibited moderate activity against the double mutant strain A(17) (K103N+Y181C) with EC(50) values lower than 5 μM. In addition, the binding modes with RT and the preliminary structure-activity relationships of these derivatives were also explored for further chemical modifications.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP91010	Benzhydrol		91-01-0	Price

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