Synthesis and HIV-1 integrase inhibition of novel bis- or tetra-coumarin analogues |
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| Authors: | Chiang Chih-Chia Mouscadet Jean-François Tsai Hou-Jen Liu Chi-Tsan Hsu Ling-Yih |
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| Affiliation: | Department of Applied Chemistry and Materials Science, Institute of Technology, National Defense University, Ta-shi, Tao-yuan, Taiwan, ROC.. |
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| Abstract: | Present studies were undertaken on the preparation of synthetic analogues of bis- or tetra-coumarins and their activity against HIV-1 integrase (HIV-1 IN). Among these coumarin analogues, compounds 14, 16 and 18 were found to be potent molecules against HIV-1 IN at IC50 values of 0.96, 0.58, and 0.49 microM, respectively. The results provided a tool for guiding the further design of more potent antiviral agents and for predicting the affinity of related compounds. |
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