Synthesis, Characterization and Cytotoxic Study of 2-Hydroxy Benzothiazole Incorporated 1,3,4-Oxadiazole Derivatives
Synthesis, Characterization and Cytotoxic Study of 2-Hydroxy Benzothiazole Incorporated 1,3,4-Oxadiazole Derivatives
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DOI：
10.21608/ejchem.2019.17265.2059
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发表时间：
2020-02-01
影响因子：
1.3
通讯作者：
Nazreen, Syed
中科院分区：
文献类型：
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作者：
Alghamdi, Afnan A.;Nazreen, Syed
合成了15个由2-羟基苯并噻唑衍生的1，3，4-恶二唑类化合物，并对其抗癌活性进行了筛选。不同的芳香酸被用于该文库以产生构效关系。针对MCF-7乳腺癌细胞进行体外细胞毒性。合成的化合物显示出可变的细胞毒性作用。4个化合物显示出较强的细胞毒作用，IC_（50）为1.8 μ M/mL ~ 4.5 μ M/mL。其他化合物显示出中度至较低的细胞毒性。2-（5-（（苯并[d]噻唑-2-基氧基）-甲基）-1，3，4-恶二唑-2-基）苯酚是最有效的化合物，其显示出与标准药物多西他赛（IC 50 1.2 +/- 0.005 μ M/mL）相当的细胞毒性作用（IC 50 1.8 +/-0.02 μ M/mL）。从结果中观察到，芳环活化基团如甲基和羟基增强了细胞毒性作用，而芳环失活基团如硝基对MCF-7乳腺癌细胞系显示出中等的细胞毒性。
A SERIES of fifteen 1, 3, 4-oxadiazoles derived from 2-hydroxy benzothiazole have been synthesized and screened for the anticancer activity. Different aromatic acids were used for this library for generating structure activity relationship. The in vitro cytotoxicity was done against MCF-7 breast cancer cells. The synthesized compounds showed variable cytotoxic effects. Four compounds showed potent cytotoxic effect with IC50 varies from 1.8 mu M/mL to 4.5 mu M/mL. Other compounds showed moderate to lower cytotoxicity. 2-(5-((benzo[d]thiazol-2-yloxy)-methyl)-1,3,4-oxadiazol-2-yl)phenol was the most potent compound which showed a cytotoxicity effect (IC50 1.8 +/- 0.02 mu M/mL) comparable to the standard drug Doxirubicin (IC50 1.2 +/- 0.005 mu M/mL). From the result it was observed that aromatic ring activating groups such as methyl and hydroxyl, enhances the cytotoxicity effect, whereas aromatic ring deactivating groups such as nitro group showed moderate cytotoxicity against MCF-7 breast cancer cell line.