Synthesis and evaluation of thiazolidinone–pyrazole conjugates as anticancer and antimicrobial agents. (30th April 2018)

• Record Type: Journal Article
• Authors: Bhat, Mahima; Poojary, Boja; Kalal, Bhuvanesh Sukhlal; Gurubasavaraja Swamy, Purawarga Matada; Kabilan, Senthamaraikannan; Kumar, Vasantha; Shruthi, Nooji; Alias Anand, Selvam Athavan; Pai, Vinitha Ramanath
• Is Part Of: Future medicinal chemistry. Volume 10:Number 9(2018)
• Page Start: 1017
• Page End: 1036
• Publication Date: 2018-04-30
• Subjects: A375 -- ADME parameters -- anticancer activity -- cytotoxicity -- HDF -- MDA-MB-231 -- MDM2 -- molecular docking -- molecular dynamics simulation -- N-arylpyrazole -- p53 -- thiazolidin-4-one; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.4155/fmc-2017-0191
• Languages: English
• ISSNs: 1756-8919

Abstract

Aim: To synthesize a series of new thiazolidinone–pyrazole hybrids (5a–o) and assess their anticancer ( in vitro and in vivo ) and antimicrobial activities.Results: The compounds5h (against Ehrlich ascites carcinoma cells), 5e and5i (against the human breast cancer [MDA-MB231] cell line) exhibited potent anticancer activity. All the compounds except5g and5e found to be less toxic for the human dermal fibroblast cells. The effective interactions of the compounds in silico with MDM2 exemplified their inhibitory potency. The derivatives also showed moderate antimicrobial activity.Conclusion: The halogen atoms on various positions of the N -arylamino ring played an advantageous role in elevating the potency of the molecules. Thus, these conjugates could be used as a lead for further optimization to achieve promising therapeutics. Graphical abstract: