title: Synthesis and biological evaluation of novel 2-imino-4-thiazolidinone derivatives as potent anti-cancer agents.
abstract: A new series of 2-imino-4-thiazolidinone derivatives (7a-7t) has been synthesised and screened for their cytotoxicity against three cancer cell lines (B16F10, A549, PANC-1) and normal cell line (CHO). Among the compounds tested, compounds 7k, 7m, 7n showed potent cytotoxicity against B16F10 cell line with IC50between 3.4 and 7μM. Interestingly these three compounds are non toxic to non cancerous CHO cells and induced apoptosis in B16F10 cells observed by DNA damage analysis through PI/Hoechst double staining method. Compounds 7k and 7n induced G0/G1 cell cycle arrest while compound 7m induced G2/M cell cycle arrest in B16F10 cells which confirms that these compounds have role in cancer cell cycle regulation. Additionally, compound 7m showed generation of intracellular reactive oxygen species (ROS) in B16F10 cells that may contribute in the cell cycle arrest whereas compounds 7k and 7n show anti-cancer activity through independent of ROS formation. Induction of apoptosis, cell cycle arrest in B16F10 cells are found to be the anti-cancer mechanism of these three compounds. The results all together demonstrate the potent cytotoxic nature of these compounds in cancer cells could be considered as new class of chemotherapeutic agents in near future.
authors.affiliation: Fluoroorganics Division, Indian Institute of Chemical Technology (CSIR-IICT), Tarnaka, Hyderabad 500007, India.
authors.forename: K
authors.initials: K
authors.lastname: Appalanaidu
authors.affiliation: Biomaterials Group, Indian Institute of Chemical Technology (CSIR-IICT), Tarnaka, Hyderabad 500007, India.
authors.forename: Rajesh
authors.initials: R
authors.lastname: Kotcherlakota
authors.affiliation: Fluoroorganics Division, Indian Institute of Chemical Technology (CSIR-IICT), Tarnaka, Hyderabad 500007, India; Government of Maharashtra's Ismail Yusuf College, Jogeshwari (E), Mumbai 400060, India.
authors.forename: T L
authors.initials: TL
authors.lastname: Dadmal
authors.affiliation: Biomaterials Group, Indian Institute of Chemical Technology (CSIR-IICT), Tarnaka, Hyderabad 500007, India.
authors.forename: Vishnu Sravan
authors.initials: VS
authors.lastname: Bollu
authors.affiliation: Fluoroorganics Division, Indian Institute of Chemical Technology (CSIR-IICT), Tarnaka, Hyderabad 500007, India. Electronic address: kumbhare@iict.res.in.
authors.forename: Ravindra M
authors.initials: RM
authors.lastname: Kumbhare
authors.affiliation: Biomaterials Group, Indian Institute of Chemical Technology (CSIR-IICT), Tarnaka, Hyderabad 500007, India. Electronic address: crpatra@iict.res.in.
authors.forename: Chitta Ranjan
authors.initials: CR
authors.lastname: Patra
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D016466:CHO Cells; D045744:Cell Line, Tumor; D006224:Cricetinae; D003412:Cricetulus; D051379:Mice; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D053778:Thiazolidines
keywords: 2-Imino-4-thiazolidinone; Apoptosis; B16F10 cell line; Cytotoxicity; Reactive oxygen species (ROS)