Synthesis, characterisation and invitro anticancer activity of thiazolidine-2,4-dione derivatives
Journal Title: Journal of Drug Discovery and Therapeutics - Year 2014, Vol 2, Issue 12
Abstract
Thiazolidine-2,4-diones exhibit broad spectrum of biological activities like antimicrobial, anticancer, anti-inflammatory, anti diabetic etc.The aim and objective of present study was to develop novel thiazolidine-2,4-diones hybrid analogues in favour of the molecular docking studies and to evaluate their cytotoxic activities. The molecular docking studies of the proposed derivatives were carried out using softwares - Argus lab, CORINA,swiss PDB and Molegro molecular viewer. The anti cancer targets used is PPAR-γ and those with better scores were selected and subjected for the wet lab synthesis. In this study, 5 novel thiazolidine-2,4-dione analogues were synthesized by the Knoevenangel condensation reaction of thiazolidine-2,4-diones with substituted aromatic aldehydes using L-Tyrosine as catalyst to yield 5-arylidine thiazolidine-2,4-diones,which on further undergo mannich reaction with aromatic amines to yield mannich bases. The purity of the newly synthesized compounds was ascertained by consistency in the TLC as well as melting point determination and was characterized by means of FTIR,1HNMR and MASS spectral analysis. Among the synthesized compounds, POD 1,POD 2, POD 3 with better scores were tested for in-vitro cytotoxicity studies by MTT assay on MCF-7 cell lines. Among this POD 1 and POD 2 exhibited significant activity on the cell line. Finally it was concluded that novel thiazolidine-2,4-diones hybrid analogues can be considered as the future lead molecule for drug discovery process.
Authors and Affiliations
T. T Akshaya*| Department of Pharmaceutical Chemistry, Devaki Amma Memorial College of Pharmacy, Pulliparamba (P.O), Chelembra, Malappuram-673634, Kerala, India, V. B Arunlal| Department of Pharmaceutical Chemistry, Devaki Amma Memorial College of Pharmacy, Pulliparamba (P.O), Chelembra, Malappuram-673634, Kerala, India, Dr. G. Babu| Department of Pharmaceutical Chemistry, Devaki Amma Memorial College of Pharmacy, Pulliparamba (P.O), Chelembra, Malappuram-673634, Kerala, India, Dr. Biju. C. R| Department of Pharmaceutical Chemistry, Devaki Amma Memorial College of Pharmacy, Pulliparamba (P.O), Chelembra, Malappuram-673634, Kerala, India
Keywords
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