Design,Synthesis, and Biological Evaluation of 1‐(thiophen‐2‐yl)‐9H‐pyrido[3,4‐b]indole Derivatives as Anti‐HIV‐1 Agents |
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| Authors: | Penta Ashok Cui‐Lin Lu Subhash Chander Yong‐Tang Zheng Sankarnarayanan Murugesan |
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| Affiliation: | 1. Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Rajasthan, India;2. Key laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan, China;3. Kunming College of Life Science, University of Chinese Academy of Sciences, Kunming, Yunnan, China |
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| Abstract: | A novel series of 1‐(thiophen‐2‐yl)‐9H‐pyrido 3,4‐b]indole derivatives were synthesized using DL‐tryptophan as starting material. All the compounds were characterized by spectral analysis such as 1H NMR, Mass, IR, elemental analysis and evaluated for inhibitory potency against HIV‐1 replication. Among the reported analogues, compound 7g exhibited significant anti‐HIV activity with EC50 0.53 μm and selectivity index 483; compounds 7e , 7i , and 7o displayed moderate activity with EC50 3.8, 3.8, and 2.8 μm and selectivity index >105, >105, and 3.85, respectively. Interestingly, compound 7g inhibited p24 antigen expression in acute HIV‐1IIIB infected cell line C8166 with EC50 1.1 μm . In this study, we also reported the Lipinski rule of 5 parameters, predicted toxicity profile, drug‐likeness, and drug score of the synthesized analogues. |
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| Keywords: |
AIDS
C8166 cells
HAART
HIV‐1 indole p24 antigen β ‐carboline |
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