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合成及含吡唑杂环的查尔酮类衍生物的生物评价作为抗癌和抗菌剂。

Synthesis and biological evaluation of a novel series of chalcones incorporated pyrazole moiety as anticancer and antimicrobial agents.

机构信息

Department of Chemistry (Biochemistry Branch), Faculty of Science, Cairo University, Giza, Egypt.

出版信息

Appl Biochem Biotechnol. 2012 Nov;168(5):1153-62. doi: 10.1007/s12010-012-9848-8. Epub 2012 Sep 5.

DOI:10.1007/s12010-012-9848-8
PMID:22948604
Abstract

A newly synthesized series of chalcone derivatives containing pyrazole rings were synthesized and evaluated for their cytotoxic activities in vitro against several human cancer cell lines. Most of the prepared compounds showed potential cytotoxicity against human breast cancer cell lines MCF-7, HEPG-2, and HCT-116. Also the compounds were evaluated as antimicrobial agents. The three compounds 3, 4, and 5 were proved to be better anticancer agents than the positive standard doxorubicin with IC50 values (4.7, 4.4, and 3.9 μg/ml) against the same human cancer cell lines, whereas compounds 5 and 6 showed the most active antimicrobial compounds in comparison to the other chalcones.

摘要

一个新合成的含有吡唑环的查尔酮衍生物系列被合成并评估了它们对几种人癌细胞系的体外细胞毒性活性。大多数制备的化合物对人乳腺癌细胞系 MCF-7、HEPG-2 和 HCT-116 表现出潜在的细胞毒性。此外,这些化合物还被评估为抗菌剂。化合物 3、4 和 5 被证明是比阳性标准阿霉素更好的抗癌剂,其对相同的人癌细胞系的 IC50 值(4.7、4.4 和 3.9μg/ml),而化合物 5 和 6 与其他查尔酮相比表现出最活跃的抗菌化合物。

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