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Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
ISSN: 1596-5996 EISSN: 1596-5996
Vol. 16, No. 8, 2017, pp. 1957-1963
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Bioline Code: pr17248
Full paper language: English
Document type: Research Article
Document available free of charge
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Tropical Journal of Pharmaceutical Research, Vol. 16, No. 8, 2017, pp. 1957-1963
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Synthesis and in vitro evaluation of novel isatinincorporated thiadiazole hybrids as potential anti-breast cancer agents
Kumar, Neeraj; Sharma, Chandra Shekhar; Singh, Hemendra Pratap & Chauhan, Lalit Singh
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
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