Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Synthesis and in vitro evaluation of novel isatin-incorporated thiadiazole hybrids as potential anti-breast cancer agents

Neeraj Kumar¹ , Chandra Shekhar Sharma², Hemendra Pratap Singh², Lalit Singh Chauhan³

¹Department of Pharmaceutical Chemistry, Geetanjali Institute of Pharmacy, Udaipur-313022; ²Department of Pharmaceutical Chemistry, B. N. College of Pharmacy, Udaipur-313001; ³Department of Pharmaceutical Sciences, Mohanlal Sukhadia University, Udaipur-313001, India.

For correspondence:- Neeraj Kumar Email: neerajkumarkamra@gmail.com

Received: 4 May 2015 Accepted: 22 April 2017 Published: 31 August 2017

Citation: Kumar N, Sharma CS, Singh HP, Chauhan LS. Synthesis and in vitro evaluation of novel isatin-incorporated thiadiazole hybrids as potential anti-breast cancer agents. Trop J Pharm Res 2017; 16(8):1957-1963 doi: 10.4314/tjpr.v16i8.28

© 2017 The authors.
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Abstract

Purpose: To synthesis and characterize some novel isatin-incorporated thiadiazoles and screen them for anti-breast cancer activity in human breast adenocarcinoma cells (MCF-7).

Method: A series of isatin incorporated Schiff bases of thiadiazoles (3a-3l) was synthesized by reaction of substituted thiadiazoles (1a-1d) with isatin (2a) and N-alkyl substituted isatin (2b-2c) and characterized by elemental analysis, IR, 1H NMR, 13C NMR and LCMS. The newly synthesized compounds were screened for their in-vitro cytotoxicity against MCF-7 cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric and Sulforhodamine B (SRB) methods.

Results: Compounds 3a, 3c, 3d, 3g and 3j showed anticancer activity in both MTT and SRB assay. Compound 3-(5-(4-chlorophenyl)-1,3,4-thiadiazol-2-ylimino)-1-ethylindolin-2-one (3g) showed most potent cytotoxic activity against MCF-7 cell lines.

Conclusion: The novel isatin incorporated thiadiazoles synthesized and characterized in this study possess anti-cancer activities in human breast adenocarcinoma cells (MCF-7). This can possibly lead to emergence of new anti-breast cancer agents.

Keywords: Thiadiazoles, Isatin, In-vitro cytotoxicity, Human breast adenocarcinoma cells (MCF-7), SRB assay