Synthesis, characterization, and biological evaluation of thiazolidine-2,4-dione derivatives

被引:14
作者
Alegaon, Shankar G. [1 ]
Alagawadi, Kallanagouda R. [1 ]
Pawar, Sneha M. [1 ]
Vinod, D. [2 ]
Rajput, Udaysingh [3 ]
机构
[1] KLE Univ, Coll Pharm, Dept Pharmaceut Chem, Belgaum 590010, Karnataka, India
[2] Madras Med Coll & Govt Gen Hosp, Coll Pharm, Dept Pharmaceut Chem, Madras, Tamil Nadu, India
[3] RL Sci Inst, Dept Chem, Belgaum 590001, Karnataka, India
关键词
Antimicrobial activity; Cytotoxic activity; Thiazolidine-2,4-dione; Drug likeliness; REDUCTASE INHIBITORY-ACTIVITY; ANTIMICROBIAL ACTIVITY; THIAZOLIDINEDIONES; 5-ARYLIDENE-2,4-THIAZOLIDINEDIONES; GAMMA;
D O I
10.1007/s00044-013-0705-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
As a part of our continuation studies in developing new derivatives as dual antimicrobial/antitumor agents we describe the synthesis of new (Z)-2-(5-arylidene-2,4-dioxothiazolidin-3-yl) acetic acid derivatives (3a-m). The chemical structures of the compound were elucidated by FTIR, H-1 NMR, C-13 NMR, and elemental analysis data. The antimicrobial activity of all products was examined. All newly synthesized compounds were tested for their in vitro anticancer activity against four cancer cell lines. Among the synthesized compounds, 3a exhibited notable activity against HeLa, HT29, A549, and MCF-7 cell lines with IC50 values of 55, 40, 38, and 50 mu M, respectively. In order to predict the drug likeliness of the synthesized compounds on the guidelines of Lipinski rule of five studies was carried out using Pallas software.
引用
收藏
页码:987 / 994
页数:8
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