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Anticancer activity of new quinolinyl–benzothiazolyl clubbed with amino acids and their in-silico studies

  • S. Shashidhar Bharadwaj,
  • Boja Poojary,
  • Sathish Kumar Boda,
  • T. Shubhavathi,
  • Vinuta Kamat,
  • Bhuvanesh Sukhlal Kalal

摘要

A lot of research is focused on creating novel chemotherapeutic medicines since cancer is becoming a more serious concern. In the present investigation, we have developed some quinolinyl–benzothiazolyl linked with amino acids and their anticancer efficacy against melanoma and breast cancer cells evaluated. All the compounds evaluated for in silico studies towards the target protein Human estrogen receptor (PDB: 2IOK). Out of all the evaluated aminoacids conjugates four compounds 5b, 5 k, 5f, and 5d exhibited remarkable docking scores and were chosen for in vitro anticancer studies. Out of which 5 k, and 5f exhibited good anticancer properties with the IC50[μg/mL] of 22.9 and 22.3 respectively against the melanoma cell line and 5b exhibited good anticancer properties with the IC50[μg/mL] of 61.0 against breast cancer cell.

Graphical Abstract