Anti-HIV-1 screening of (2E)-3-(2-chloro-6-methyl/methoxyquinolin-3-yl)-1-(aryl)prop-2-en-1-ones

作者：Rizvi Syed Umar Farooq; Ahmad Matloob^*; Bukhari Mujahid Hussain; Montero Catherine; Chatterjee Payel; Detorio Mervi; Schinazi Raymond F

来源：Medicinal Chemistry Research, 2014, 23(1): 402-407.

DOI：10.1007/s00044-013-0652-y

• Heterocyclic compounds
• Quinolyl chalcones
• Arylketone
• Cytotoxicity
• Anti-HIV-1 activity

Biological studies of two series of 38 quinolinyl chalcones (4a-s and 5a-s) were investigated for their in vitro anti-HIV-1 and cytotoxic activities. Out of 38 compounds, seventeen compounds were observed as good anti-HIV-1 agents with EC50 values less than 20 mu M. Compounds 4a, 4l, 4o, 5e, 5h, 5l, 5o, and 5r displayed potent anti-HIV-1 activity with EC50 values less than 5 mu M. Among these, compound 5h emerged as the best anti-HIV-1 agent (EC50 = 1.1 mu M). Compounds 4d, 4n, 4q, 4r, 4s, 5n, and 5r showed no toxicity in human lymphocytes. Bioassay results show that the type(s) and position(s) of the substituents seem to be critical for their cytotoxic and anti-HIV-1 activities. These results could be useful in the invention of new anti-HIV agents through structural modification.

• 出版日期2014-1