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Design, synthesis, in-silico study and anticancer potential of novel n-4- piperazinyl-ciprofloxacin-aniline hybrids

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dc.contributor.author Akhtar, Rabia
dc.contributor.author Zahoor, Ameer Fawad
dc.contributor.author Rasul, Azhar
dc.contributor.author Ahmad, Matloob
dc.contributor.author Anjum, Muhammad Naveed
dc.contributor.author Ajmal, Muhammad
dc.contributor.author Raza, Zohaib
dc.date.accessioned 2022-12-05T05:17:02Z
dc.date.available 2022-12-05T05:17:02Z
dc.date.issued 2019-09-02
dc.identifier.citation Akhtar, R., Zahoor, A. F., Rasul, A., Ahmad, M., Anjum, M. N., Ajmal, M., & Raza, Z. (2019). Design, synthesis, in-silico study and anticancer potential of novel n-4-piperazinyl-ciprofloxacin-aniline hybrids. Pak. J. Pharm. Sci, 32(5), 2215-2222. en_US
dc.identifier.issn 1011-601X
dc.identifier.uri http://142.54.178.187:9060/xmlui/handle/123456789/14616
dc.description.abstract Synthesis and characterization of novel structural hybrids of ciprofloxacin linked with a variety of anilides have been described in this paper. Antitumor activity of these derivatives was assessed against liver cell line (Huh-7) using MTT assay. Among the synthesized derivatives, compound 6a inhibited the growth of tumor cells by displaying 68.36% cell viability at 100 µg/mL concentration which was then in-silico modelled to delineate the potential mechanistic insights for its antiproliferative activity. The PASS prediction indicated the TopII as potential anticancer target of compound 6a. The induced fit docking revealed that compound 6a inhibits the TopII with superior binding affinity and forms stronger contacts with active site’s key residues responsible for DNA-TopII intercalation and catalytic inhibition consistent with its cytotoxic potential. Therefore, compound 6a can be considered as a potential lead for further optimization in the development of ciprofloxacin-derived anticancer drugs. en_US
dc.language.iso en en_US
dc.publisher Karachi: Faculty of Pharmacy & Pharmaceutical Sciences, Karachi en_US
dc.subject Fluoroquinolones en_US
dc.subject cytotoxic activity en_US
dc.subject human liver cell line en_US
dc.subject anti-cancer en_US
dc.subject induced fit docking en_US
dc.title Design, synthesis, in-silico study and anticancer potential of novel n-4- piperazinyl-ciprofloxacin-aniline hybrids en_US
dc.type Article en_US


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