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SYNTHESIS AND CYTOTOXIC EVALUATION OF 2-AMINOBENZOTHIAZOLE DERIVATIVES. Rupinder Kaur Gill, P. M. S. Bedi.

SYNTHESIS AND CYTOTOXIC EVALUATION OF 2-AMINOBENZOTHIAZOLE DERIVATIVES.

Rupinder Kaur Gill, P. M. S. Bedi.

International Journal of Natural Product Science 2012: Spl Issue 1:100.

Abstract(RBIP-100)

To develop drugs with selective action, current research mainly focuses on different aspects of cancer biology such as therapeutic intracellular targets involved in cell proliferation. Naturally occurring and synthetic benzothiazoles display significant inhibitory activity against topoisomerase II, tyrosine kinase, Clk 1/4, ubiquitin proteasome system and have antiproliferative activities in a variety of cell lines.1-3 Therefore, we have synthesized a series of N-bromoalkyl-benzothiazol-2-yl-amine derivatives and evaluate in vitro cytotoxic activity against four different human cancer cell lines namely Lung: A-549, Prostate: PC-3, Leukemia: THP-1 and Colon: Caco-2 at 10, 50 and 100 µM concentrations.



The benchmark active compound 1 (X2 = OCH3, X = X1 = H, n = 3) shows IC50 value of 0.6 µM, 3 µM and 9.9 µM against prostate, leukemia and colon cancer cell lines respectively. Other active analogues (X2 = F, X = X1 = H, n = 3 and X = Cl, X1 = X2 = H, n = 3) showed IC50 value of 3.5 µM, 0.9 µM and 3.5 µM, 1.72 µM against prostate and leukemia cancer cell line respectively.
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