Microwave-assisted synthesis and antitumor evaluation of a new series of thiazolylcoumarin derivatives. Academic Article uri icon

Overview

abstract

  • A new series of thiazolylcoumarin derivatives was synthesized. The designed strategy embraced a molecular hybridization approach which involves the combination of the thiazole and coumarin pharmacophores together. The new hybrid compounds were tested for in vitro antitumor efficacy over cervical (Hela) and kidney fibroblast (COS-7) cancer cells. Compounds 5f, 5h, 5m and 5r displayed promising efficacy toward Hela cell line. In addition, 5h and 5r were found to be the most active candidates toward COS-7 cell line. The four active analogs, 5f, 5h, 5m and 5r were screened for in vivo antitumor activity over EAC cells in mice, as well as in vitro cytotoxicity toward W138 normal cells. Results illustrated that 5r has the highest in vivo activity, and that the four analogs are less cytotoxic than 5-FU toward W138 normal cells. In this study, 3D pharmacophore analysis was performed to investigate the matching pharmacophoric features of the synthesized compounds with trichostatin A. In silico studies showed that the investigated compounds meet the optimal needs for good oral absorption with no expected toxicity hazards.

publication date

  • August 30, 2017

Identity

PubMed Central ID

  • PMC5735336

Scopus Document Identifier

  • 85029612347

Digital Object Identifier (DOI)

  • 10.17179/excli2017-208

PubMed ID

  • 29285008

Additional Document Info

volume

  • 16