MICROWAVE ASSISTED SYNTHESIS AND MOLECULAR MODELING STUDIES OF SOME NOVEL POLO-LIKE KINASE 1 INHIBITORS AS ANTICANCER AND ANTI-INFLAMMATORY AGENTS

Authors

  • Ganesh K. Dhikale
  • Ramesh L. Sawant
  • Mahesh R. Dumbare

Keywords:

1, 3 – thiazolidin – 4 – one, Anti-cancer activity, Anti-inflammatory activity, Molecular Modeling, Polo-like kinase 1

Abstract

A series of 1, 3-thiazolidin-4-one analogues were synthesized using microwave and structurally characterized by various spectroscopic techniques and elemental analysis. All synthesized compounds were screened for anticancer activity by sulforhodamine B (SRB) assay while in vitro anti-inflammatory activity was by inhibition of albumin denaturation technique. The compounds 5j, 5k, 5l, 5m, 5n were found to show significant anticancer and in vitro anti-inflammatory activity. Furthermore, molecular modelling studies of all molecules (5a-5s) were performed using V Life MDS software. Based on this it is observed that, compound 5m shows more stable complex with Polo-like kinase 1 by forming hydrogen bond and hydrophobic interactions. Finally it is concluded that, 1, 3-thiazolidin-4-one analogues shows anticancer and anti-inflammatory activity possibly because of inhibition of Polo- like kinase 1.

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Published

02-04-2020