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铜催化的氨基萘醌-磺酰脒共轭物的三组分合成及其抗增殖活性的体外评价。

Copper-catalyzed three-component synthesis of aminonaphthoquinone-sulfonylamidine conjugates and in vitro evaluation of their antiproliferative activity.

作者信息

Suja Thachapully D, Divya K V L, Naik Lakshma V, Ravi Kumar A, Kamal Ahmed

机构信息

Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.

Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.

出版信息

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2072-6. doi: 10.1016/j.bmcl.2016.02.071. Epub 2016 Feb 26.

DOI:10.1016/j.bmcl.2016.02.071
PMID:26948541
Abstract

A series of aminonaphthoquinone-sulfonylamidine conjugates were synthesized via a copper-catalyzed three-component reaction of N-propargyl aminonaphthoquinone, sulfonyl azides and various amines. Majority of the compounds exhibited promising antiproliferative potential when evaluated against a panel of four cancer cell lines. Docking experiments of representative compounds indicated that the conjugates can occupy the ATP-binding pocket of topoisomerase-II enzyme.

摘要

通过N-炔丙基氨基萘醌、磺酰叠氮化物和各种胺的铜催化三组分反应合成了一系列氨基萘醌-磺酰脒共轭物。当针对一组四种癌细胞系进行评估时，大多数化合物表现出有前景的抗增殖潜力。代表性化合物的对接实验表明，这些共轭物可以占据拓扑异构酶-II酶 的ATP结合口袋。

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