点击次数：

论文类型：期刊论文

第一作者：Li, Yingjun

通讯作者：Li, YJ (reprint author), Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Peoples R China.

合写作者：Yu, Yang,Jin, Kun,Gao, Lixin,Luo, Tongchuan,Sheng, Li,Shao, Xin,Li, Jia

发表时间：2014-09-01

发表刊物：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

收录刊物：SCIE、PubMed、Scopus

卷号：24

期号：17

页面范围：4125-4128

ISSN号：0960-894X

关键字：Thiadiazole amides; Cdc25B; PTP1B; Cancer; Type-2 diabetes and obesity

摘要：A series of novel thiadiazole amide derivatives have been synthesized and evaluated for inhibitory activities against Cdc25B and PTP1B. Most of them showed inhibitory activities against Cdc25B (IC50 = 1.18-8.01 mu g/mL) and PTP1B (IC50 = 0.85-8.75 mu g/mL), respectively. Moreover, compounds 5b and 4l were most potent with IC50 values of 1.18 and 0.85 mu g/mL for Cdc25B and PTP1B, respectively, compared with reference drugs Na3VO4 (IC50 = 0.93 mu g/mL) and oleanolic acid (IC50 = 0.85 mu g/mL). The results of selectivity experiments showed that the target compounds were selective inhibitors against PTP1B and Cdc25B. Enzyme kinetic experiments demonstrated that compound 5k was a specific inhibitor with the typical characteristics of a mixed inhibitor. (C) 2014 Elsevier Ltd. All rights reserved.