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Synthesis, Anti-Hiv-1 and Antiproliferative Evaluation of Novel 4-Nitroimidazole Derivatives Combined With 5-Hydroxy-4-Pyridinone Moiety Publisher



Shirvani P1 ; Fassihi A1, 2 ; Saghaie L1 ; Van Belle S3 ; Debyser Z3 ; Christ F3
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Hezar Jerib, 817416-73461, Isfahan, Iran
  2. 2. Bioinformatics Research Center, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, 81746-73461, Isfahan, Iran
  3. 3. Department of Pharmacological and Pharmaceutical Sciences, Laboratory of Molecular Virology and Gene Therapy, KU Leuven, Belgium

Source: Journal of Molecular Structure Published:2020


Abstract

In an effort to synthesize more effective non-nucleoside reverse transcriptase inhibitors (NNRTIs) against the HIV-1 infection, a new series of novel 4-nitroimidazole derivatives combined with 5-hydroxy-4-pyridinone moiety were designed by molecular docking studies, prepared and characterized by spectroscopic techniques. All the synthesized compounds were in vitro evaluated for their inhibitory effect against the HIV-1 replication in the MT-4 cells. Results showed that none of these synthesized compounds displayed any specific anti HIV-1 activity. Surprisingly, these compounds showed high cytotoxicity against MT-4 cells with low selectivity index (<1), therefore could be new potential antiproliferative agents. Therefore, their antiproliferative property were evaluated against MOLM-13 and K562 (leukemia) cell lines. Compound 14g showed notable antitumor activity toward both studied cell lines (EC50 = 1.3 μM and EC50 = 1.8 μM respectively). © 2019 Elsevier B.V.
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