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噻吩并[2,3-d]嘧啶-4-酮衍生物在药物化学中的最新进展,重点关注其合成及抗癌特性。

Recent developments regarding the use of thieno[2,3-d]pyrimidin-4-one derivatives in medicinal chemistry, with a focus on their synthesis and anticancer properties.

作者信息

Bozorov Khurshed, Zhao Jiang-Yu, Elmuradov Burkhon, Pataer Apar, Aisa Haji A

机构信息

Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, South Beijing Road 40-1, Urumqi, Xinjiang 830011, PR China; Institute of the Chemistry of Plant Substances, Academy of Sciences of Uzbekistan, 77, Mirzo Ulugbek Str., 100170 Tashkent, Uzbekistan.

Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, South Beijing Road 40-1, Urumqi, Xinjiang 830011, PR China.

出版信息

Eur J Med Chem. 2015 Sep 18;102:552-73. doi: 10.1016/j.ejmech.2015.08.018. Epub 2015 Aug 13.

DOI:10.1016/j.ejmech.2015.08.018
PMID:26312434
Abstract

It is generally understood that the antitumor properties of synthetic heterocyclic compounds are among the most powerful properties that can be made use in medicinal chemistry. More specifically, their substantial cytotoxic effects against different types of human tumor cells, in addition to their roles as enzymes or receptors for various kinase inhibitors, make them critically important. In recent years, thieno[2,3-d]pyrimidin-4-one derivatives (TPs), which are analogs of quinazoline alkaloids, have frequently attracted the interest of medicinal chemistry researchers due to their promising anticancer properties. The present study is a review of the latest advances (i.e., since 2006) in TP derivative-related research, with a focus on how such derivatives are synthesized and on their anticancer activities.

摘要

人们普遍认为,合成杂环化合物的抗肿瘤特性是药物化学中可利用的最强大特性之一。更具体地说,它们对不同类型人类肿瘤细胞具有显著的细胞毒性作用,此外,它们作为各种激酶抑制剂的酶或受体,使其变得至关重要。近年来,作为喹唑啉生物碱类似物的噻吩并[2,3-d]嘧啶-4-酮衍生物(TPs),因其具有良好的抗癌特性,经常引起药物化学研究人员的兴趣。本研究是对TP衍生物相关研究(即自2006年以来)的最新进展的综述,重点关注此类衍生物的合成方法及其抗癌活性。

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