Synthesis and Structure-Activity Relationship Study of 1-Phenyl-1-(quinazolin-4-yl)ethanols as Anticancer Agents

被引：37

作者：

Kuroiwa, Kenta ^{[1
]}

Ishii, Hirosuke ^{[2
]}

Matsuno, Kenji ^{[2
]}

Asai, Akira ^{[2
]}

Suzuki, Yumiko ^{[1
]}

机构：

[1] Sophia Univ, Fac Sci & Technol, Dept Mat & Life Sci, Chiyoda Ku, Tokyo 1028554, Japan

[2] Univ Shizuoka, Grad Sch Pharmaceut Sci, Suruga Ku, Shizuoka 4228526, Japan

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2015年 / 6卷 / 03期

关键词：

Quinazoline; anticancer; tubulin inhibitor; colchicine binding site; structure-activity relationship study; TUBULIN; QUINAZOLINES; COLCHICINE; DISCOVERY; BINDING;

D O I：

10.1021/ml5004684

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A quinazoline derivative PVHD121 (1a) was shown to have strong antiproliferative activity against various tumor-derived cell lines, including A549 (lung), NCI-H460 (lung), HCT116 (colon), MCF7 (breast), PC3 (prostate), and HeLa (cervical) cells with IC50 values from 0.1 to 0.3 mu M. A structure activity relationship (SAR) study at the 2- and 4-position of the quinazoline core lead to the discovery of more potent anticancer agents (14, 16, 17, 19, 24, and 31). The results of an in vitro tubulin polymerization assay and fluorescent based colchicine site competition assay with purified tubulin indicated that la inhibits tubulin polymerization by binding to the colchicine site.

引用

页码：287 / 291

页数：5

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