Design and synthesis of certain novel arylidene thiazolidinone derivatives as anticancer agents

Research Abstract

New 5-subistituted-4-thiazolidinone derivatives 4a-g were synthesized through chloroacetylation of 2-amino-benzothiazole derivatives and further cyclyised by the use of ammonium thiocyanate then subjected to different aryl and heteroaryl aldehydes. All the prepared compounds were evaluated for their antitumor activity against human breast (MCF-7) and non-small cell lung (A549) cancer cell lines. Most of compounds showed moderate antitumor activity especially the 5-(2-thiophen-arylidene)-4-thiazolidinone derivative 4a with IC50 13.25 µM against human breast MCF-7 cell line and 12.08 µM against non-small cell lung A549 cell line. Also, 5-(2-methoxy-arylidene)-4-thiazolidinone derivative 4b have the antitumor activity with IC50 14.51 µM against MCF-7 cell line and 13.25 µM against A549 cell line. All the prepared compounds were docked against EGFR using 4-anilinoquinazoline inhibitor (4AQ) (PDB ID: IM17) in away to explore their binding mode.

Research Keywords

benzothiazole-thiazolidinone