Novel glitazones: glucose uptake and cytotoxic activities, and structure-activity relationships

被引：8

作者：

Kumar, B. R. Prashantha ^{[1
]}

Kumar, S. Santhosh ^{[1
]}

Viral, Patel ^{[1
]}

Wadhwani, Ashish ^{[1
]}

Vadivelan, R. ^{[1
]}

Kumar, M. N. Satish ^{[1
]}

Elango, K. ^{[1
]}

Nanjan, M. J. ^{[1
]}

机构：

[1] JSS Coll Pharm, Ootacamund 643001, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2012年 / 21卷 / 09期

关键词：

Diabetes; glitazones; Glucose uptake; PPAR-gamma; thiazolidinediones; Cytotoxic activity; ANTIHYPERGLYCEMIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; ANTIDIABETIC AGENTS; HYPOGLYCEMIC AGENTS; INSULIN-RESISTANCE; SERUM GLUCOSE; DERIVATIVES; CANCER; THIAZOLIDINEDIONES; CIGLITAZONE;

D O I：

10.1007/s00044-011-9792-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this article, two series of novel glitazones are reported for their synthesis, in vitro glucose uptake activity by the rat hemi-diaphragm, and in vitro cytotoxic activity against human carcinoma HEp-2 (epidermoid carcinoma of the larynx) and A549 (human lung cancer cell line) cells. Some of the compounds exhibit good glucose uptake and cytotoxic activities. Compound 5 with 2,4-dichlorophenol moiety connected to TZD via the two carbon linker has exhibited good glucose uptake activity. One of the compounds exhibits both cytotoxic and glucose uptake activities (compound 4). Illustrations about their synthesis, and in vitro glucose uptake and cytotoxic activities are described along with their structure-activity relationships. Designed, synthesized some novel glitazones and evaluated them for their glucose uptake and cytotoxic activities.

引用

页码：2689 / 2701

页数：13

共 29 条

[1] Novel inhibitors of an emerging target in Mycobacterium tuberculosis;: Substituted thiazolidinones as inhibitors of dTDP-rhamnose synthesis [J].