萘并呋喃醌衍生物：对受体酪氨酸激酶的抑制作用

Naphthofuroquinone derivatives: inhibition of receptor tyrosine kinases.

作者信息

Lee Kee-In, Park Youmie, Park Su-Jin, Hwang Jung-Hwan, Lee Sung-Jin, Kim Gun-Do, Park Woo-Kyu, Lee Sunghou, Jeong Daeyoung, Kong Jae-Yang, Kang Hee-Kyoung, Cho Heeyeong

机构信息

Division of Bio-Organic Science, Korea Research Institute of Chemical Technology, Daejeon 305-353, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2006 Feb;16(3):737-42. doi: 10.1016/j.bmcl.2005.08.115.

DOI:10.1016/j.bmcl.2005.08.115

PMID:16321529

Abstract

A series of dinaphtho[1,2-b;2',3'-d]furan-7,12-dione derivatives were synthesized and evaluated for inhibitory activities against receptor tyrosine kinases. The naphthofuroquinone compounds with dialkylaminoethoxy group at C(5)-position (7, 8, 10, and 11) manifested strong inhibitory activities against epidermal growth factor receptor and vascular endothelial growth factor receptor. Docking study of 11 with EGFR was also performed.

摘要

合成了一系列二萘并[1,2 - b;2',3'- d]呋喃 - 7,12 - 二酮衍生物，并对其抑制受体酪氨酸激酶的活性进行了评估。在C(5)位带有二烷基氨基乙氧基的萘并呋喃醌化合物（7、8、10和11）对表皮生长因子受体和血管内皮生长因子受体表现出较强的抑制活性。还对化合物11与表皮生长因子受体进行了对接研究。