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

被引：27

作者：

Murty, M. S. R. ^{[1
]}

Rao, B. Ramalingeswara ^{[1
]}

Katiki, Mohana Rao ^{[1
]}

Nath, Lekshmi R. ^{[2
]}

Anto, Ruby John ^{[2
]}

机构：

[1] Indian Inst Chem Technol, Discovery Lab, Med Chem & Pharmacol Div, Hyderabad 500007, Andhra Pradesh, India

[2] Rajiv Gandhi Ctr Biotechnol, Div Canc Res, Canc Res Program, Thiruvananthapuram 695014, Kerala, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 10期

关键词：

Piperazine; Benzothiazole; Benzoxazole; 1,3,4-Oxadiazole; Anticancer; MTT assay; TERMINAL AMIDE FRAGMENT; IN-VITRO; NEW-MODEL; POTENT; DISCOVERY; RECEPTOR; 2-(4-AMINOPHENYL)BENZOTHIAZOLES; ARYLPIPERAZINES; REPLACEMENTS; SELECTIVITY;

D O I：

10.1007/s00044-013-0510-y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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), HepG(2) (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, HepG(2) and HeLa.

引用

页码：4980 / 4991

页数：12

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