title: Synthesis and in vitro evaluation of some isatin-thiazolidinone hybrid analogues as anti-proliferative agents.
abstract: A range of isatin-thiazolidinone hybrid analogues were synthesized and their cytotoxicity was evaluated against several cancer cell lines in vitro. The acute toxicity studies in mice models revealed that these analogues possess low systemic toxicity and are safe up to 1600mg/Kg. Among the compounds synthesized, 5-(2-nitrobenzylidene)-2-(isatin-3-azino)-thiazolidin-4-one (CI) has been shown to be the most active, highly promising compound which induced S phase arrest in cell cycle in a time dependent manner. Our initial analysis indicate that incorporation of electron withdrawing group at ortho position of the ring favors over the meta and para positions for eliciting its cytostatic effect. Overall, the in vitro biological evaluation suggests that the growth inhibitory effect of CI is promising and can be studied further.
authors.affiliation: Integrated Cancer Research Programme, Rajiv Gandhi Centre for Biotechnology, Thiruvananthapuram, Índia.
authors.forename: P K
authors.initials: PK
authors.lastname: Ramshid
authors.forename: Sankar
authors.initials: S
authors.lastname: Jagadeeshan
authors.forename: Anand
authors.initials: A
authors.lastname: Krishnan
authors.forename: Mary
authors.initials: M
authors.lastname: Mathew
authors.forename: S Asha
authors.initials: SA
authors.lastname: Nair
authors.forename: M Radhakrishna
authors.initials: MR
authors.lastname: Pillai
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D007510:Isatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D023382:Toxicity Tests, Acute
chemical_list: D000970:Antineoplastic Agents; D053778:Thiazolidines; D007510:Isatin