Synthesis, evaluation and docking studies on steroidal pyrazolones as anticancer and antimicrobial agents |
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Authors: | Shamsuzzaman Ashraf Mashrai Anis Ahmad Ayaz Mahmood Dar Hena Khanam Mohd Danishuddin Asad U Khan |
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Institution: | 1. Department of Chemistry Aligarh Muslim University, Aligarh, 202 002, India 2. Interdisciplinary Unit of Biotechnology Aligarh Muslim University, Aligarh, 202 002, India
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Abstract: | A series of new steroidal pyrazolones have been synthesized, characterised and evaluated for their in vitro anticancer activity. They were tested against five cancer (SW480, HepG2, A549, HeLa and HL-60) cell lines. The synthesized compounds showed high selectivity and compound 4 showed the strongest inhibitory activity against human SW480 (IC50 = 11.67 μmol L?1). In addition, the synthesized compounds were tested for their antimicrobial activity by disc diffusion assay and MIC by broth micro dilution method against Gram-positive, Gram-negative strains of bacteria as well as fungus strains and we found a correlation between the observed and predicted antimicrobial activities. Docking studies were performed to investigate the hypothetical binding mode of the target compounds. This study provided a new molecular scaffold for the further development of anticancer as well as antimicrobial agents. |
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