کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10582661 | 981085 | 2011 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of (±)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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 EC50 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 EC50 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 A17 (K103N + Y181C) with EC50 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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 16, 15 August 2011, Pages 4704-4709
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 16, 15 August 2011, Pages 4704-4709
نویسندگان
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,