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靶向酪氨酸激酶的喹喔啉类骨架及其潜在抗癌活性

Quinoxaline-Based Scaffolds Targeting Tyrosine Kinases and Their Potential Anticancer Activity.

作者信息

El Newahie Aliya M S, Ismail Nasser S M, Abou El Ella Dalal A, Abouzid Khaled A M

机构信息

Faculty of Pharmacy, Department of Pharmaceutical Organic Chemistry, October University for Modern Science and Arts (MSA), Cairo, Egypt.

Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Department of Pharmaceutical Chemistry, Future University, Cairo, Egypt.

出版信息

Arch Pharm (Weinheim). 2016 May;349(5):309-26. doi: 10.1002/ardp.201500468. Epub 2016 Apr 9.

DOI:10.1002/ardp.201500468
PMID:27062086
Abstract

Quinoxaline derivatives, also called benzopyrazines, are an important class of heterocyclic compounds. Quinoxalines have drawn great attention due to their wide spectrum of biological activities. They are considered as an important basis for anticancer drugs due to their potential activity as protein kinase inhibitors. In this review, we focus on the chemistry of the quinoxaline derivatives, the strategies for their synthesis, their potential activities against various tyrosine kinases, and on the structure-activity relationship studies reported to date.

摘要

喹喔啉衍生物,也称为苯并吡嗪,是一类重要的杂环化合物。喹喔啉因其广泛的生物活性而备受关注。由于它们作为蛋白激酶抑制剂的潜在活性,它们被认为是抗癌药物的重要基础。在这篇综述中,我们重点关注喹喔啉衍生物的化学、其合成策略、它们对各种酪氨酸激酶的潜在活性,以及迄今为止报道的构效关系研究。

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