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Synthesis of piperazinylbenzothiazole/benzoxazole derivatives coupled with 1, 3, 4-oxadiazole-2-thiol: novel hybrid heterocycles as anticancer agents

Publication Type : Journal Article

Publisher : Medicinal Chemistry Research.

Source : Medicinal Chemistry Research. 2013 Oct 1;22(10):4980-91

Url :

Campus : Kochi

School : School of Pharmacy

Center : Research & Projects

Department : Pharmacognosy

Verified : Yes

Year : 2013

Abstract : The synthesis of a series of substituted 2-(piperazin-1-yl)benzothiazole/benzoxazole coupled with 1,3,4-oxadiazole-2-thiol pharmacophore (8a–t) is described using a three carbon spacer (Jones and Helm, Drugs 69:1903–1910, 2009). The structures of the compounds were confirmed by NMR and mass spectral data. All the synthesized compounds have been evaluated for their cytotoxicity towards five human cancer cell lines of different origins, viz. MCF-7 (Breast), HeLa (Cervical), HepG2 (Liver), A431 (Skin) and A549 (Lung), and IC50 values were determined. Among the compounds tested, 8j and 8t displayed maximum cytotoxic activity. A431 was the most sensitive cell line against the compounds studied, followed by MCF7, A549,

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