title: Novel series of coumarinyl substituted-thiazolidin-2,4-dione analogs as anticancer agents: design, synthesis, spectral studies and cytotoxicity evaluation.
abstract: In this research work, a series of eighteen novel coumarinyl substituted thiazolidin-2,4-dione analogs (4a-4r) have been designed by molecular hybridization approach, synthesized and their structures were established on the basis of FTIR, 1H NMR, 13C NMR and elemental (CHN) analysis. These title compounds were screened for their cytotoxicity using MTT assay methodology against five different mammalian cancer cell lines viz. hormone dependant breast adenocarcinoma (MCF7), cervical carcinoma (HeLa), colorectal carcinoma (HT29), lung cancer (A549) and prostate adeno carcinoma (PC3). The cytotoxicity screening studies revealed that MCF-7, HeLa and A549 cancer cell lines were sensitive to all the tested compounds. Though the compounds showed varying degrees of cytotoxicity in the tested cell lines, most significant effect was observed for compounds 4i (1.06, 2.4 and 3.06 µM) and 4o (0.95, 3.2 and 2.38 μM) against MCF7, HeLa and A549 cell lines respectively. In conclusion, the anticancer results of these promising leads strongly encouraged us for additional lead optimization with the aim of developing more potential anticancer agents.
authors.affiliation: Department of Pharmaceutical Chemistry, K.L.E. University College of Pharmacy, Vidyanagar, Hubballi-580 031, Karnataka, India. palkar@ukzn.ac.za.
authors.forename: Mahesh B
authors.initials: MB
authors.lastname: Palkar
authors.forename: Sunil S
authors.initials: SS
authors.lastname: Jalalpure
authors.forename: Rajesh A
authors.initials: RA
authors.lastname: Rane
authors.forename: Harun M
authors.initials: HM
authors.lastname: Patel
authors.forename: Mahamadhanif S
authors.initials: MS
authors.lastname: Shaikh
authors.forename: Girish A
authors.initials: GA
authors.lastname: Hampannavar
authors.forename: Wesam S
authors.initials: WS
authors.lastname: Alwan
authors.forename: Girish S
authors.initials: GS
authors.lastname: Bolakatti
authors.forename: Rajshekhar
authors.initials: R
authors.lastname: Karpoormath
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D019073:HT29 Cells; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells; D009682:Magnetic Resonance Spectroscopy; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D003374:Coumarins; D045162:Thiazolidinediones; C500090:thiazolidine-2,4-dione