4.6 Article

1H-1,2,3-Triazole Tethered Nitroimidazole-Isatin Conjugates: Synthesis, Docking, and Anti-Proliferative Evaluation against Breast Cancer

Journal

ACS OMEGA
Volume 3, Issue 9, Pages 12106-12113

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsomega.8b01513

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Funding

  1. Council of Scientific and Industrial Research (CSIR), New Delhi [02IJ0293)/17/EMR-I]
  2. National Research Foundation of South Africa [UID: 99563]

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1H-1,2,3-Triazole tethered imidazole-isatin and imidazole-isatin-thiosemicarbazone conjugates were synthesized and evaluated against MCF-7 and MDA-MB-231 cell lines. Antiproliferative activities of the synthesized conjugates revealed an optimum combination of longer alkyl chain length as spacer and a halogen-substituent on the isatin ring as a prerequisite for good activity. The compound 6g with an optimum combination of chloro-substituent at C-5 position of isatin ring and a butyl chain length proved to be most active and noncytotoxic with IC50s of 54.25 and 26.12 mu M against MCF-7 and MDA-MB-231 cell lines, respectively.

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