1. 1-Aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro
- Author
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Cheng, Pi, Huang, Ning, Jiang, Zhi-Yong, Zhang, Quan, Zheng, Yong-Tang, Chen, Ji-Jun, Zhang, Xue-Mei, and Ma, Yun-Bao
- Subjects
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TETRAHYDROISOQUINOLINES , *ANTIVIRAL agents , *HIV infections , *THERAPEUTICS , *RING formation (Chemistry) - Abstract
Abstract: A series of 1-aryl-6,7-dihydroxyl(methoxy)-1,2,3,4-tetrahydroisoquinolines (compounds 1–36) were synthesized via Pictet–Spengler cyclization. All the synthesized compounds were assayed for activities against HIV-1IIIB in C8166 cell cultures by MTT method for the first time. The results of the anti-HIV screening revealed that 6,7-dihydroxytetrahydroisoquinolines possessed higher selective index than 6,7-dimethoxyl analogs due to the significantly decreased cytotoxicities. Compounds 6, 24, and 36 showed potent anti-HIV activities with EC50 values of 8.2, 4.6, and 5.3μM respectively, and the cytotoxicities (CC50) of these three compounds were 784.3, 727.3, and 687.3μM, which resulted in SI values larger than 95, 159, and 130 respectively. [Copyright &y& Elsevier]
- Published
- 2008
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