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Molecules 2006, 11(5), 325-333; doi:10.3390/11050325

Synthesis and Antitumor Evaluation of Novel Derivatives of 6-Amino-2-phenylbenzothiazoles

Received: 4 April 2006 / Revised: 20 April 2006 / Accepted: 24 April 2006 / Published: 9 May 2006
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Novel derivatives of 6-amino-2-phenylbenzothiazole bearing differentsubstituents (amino, dimethylamino or fluoro) on the phenyl ring were prepared as thecorresponding hydrochloride salts. 6-Nitro-2-(substituted-phenyl)benzothiazoles (1-6) weresynthesized by condensation reactions of substituted benzaldehydes with 2-amino-5-nitrothiophenol. Nitro derivatives were reduced to the amino derivatives with SnCl2/HCl.Water soluble hydrochloride salts of 6-amino-2-(substituted-phenyl)benzothiazole (13-19)were prepared using concentrated or gaseous HCl. Compounds 13-19 were found to exertcytostatic activities against malignant human cell lines: cervical (HeLa), breast (MCF-7),colon (CaCo-2), laryngeal carcinoma (Hep-2), and normal human fibroblast cell lines (WI-38).
Keywords: Benzothiazole synthesis; antitumor activity. Benzothiazole synthesis; antitumor activity.
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Racane, L.; Stojkovic, R.; Tralic-Kulenovic, V.; Karminski-Zamola, G. Synthesis and Antitumor Evaluation of Novel Derivatives of 6-Amino-2-phenylbenzothiazoles. Molecules 2006, 11, 325-333.

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