Synthesis and evaluation of the diarylthiourea analogs as novel anti-cancer agents

被引：17

作者：

Liu, Shengquan ^{[1
]}

Louie, Maggie C. ^{[1
,3
]}

Rajagopalan, Vanishree ^{[1
]}

Zhou, Guangyan ^{[2
]}

Ponce, Esmeralda ^{[3
]}

Nguyen, Tran ^{[1
]}

Green, Linda ^{[3
]}

机构：

[1] Touro Univ Calif, Coll Pharm, Vallejo, CA 94592 USA

[2] Touro Univ Calif, Dept Basic Sci, Vallejo, CA 94592 USA

[3] Dominican Univ Calif, Dept Nat Sci & Math, San Rafael, CA 94901 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 06期

关键词：

SHetA2; Diarylthiourea analogs; Anticancer agents; Breast cancer; Prostate cancer; HETEROAROTINOIDS; SHETA2; UREA;

D O I：

10.1016/j.bmcl.2015.01.042

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Ten p-nitrodiarylthiourea analogs were designed, synthesized and evaluated in breast (MCF-7, T-47D, MDA-MB-453) and prostate (DU-145, PC-3, LNCaP) cancer cell lines for their anticancer activities. The majority of the compounds were able to inhibit the growth of these six cancer cell lines at low micromolar concentrations. Compound 7 was found to be the most potent anticancer agent in this series with GI(50) values of 3.16 mu M for MCF-7, 2.53 mu M for T-47D, 4.77 mu M for MDA-MB-453 breast cancer lines and 3.54 mu M for LNCaP prostate cancer cell line. These GI(50) values were comparable to the parent compound, SHetA2. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：1301 / 1305

页数：5

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