Synthesis, anticancer, and molecular docking studies of pyranone derivatives

被引：9
|
作者：
Swamy, P. M. Gurubasavaraja [1 ]
Sri, B. Ramya [1 ]
Giles, D. [1 ]
Shashidhar, B. V. [1 ]
Das, Amit Kumar [1 ]
Agasimundin, Y. S. [2 ]
机构：
[1] Acharya & BM Reddy Coll Pharm, Med Chem Res Lab, Bangalore 560090, Karnataka, India
[2] SCS Coll Pharm, Med Chem Res Lab, Harapanahalli 583131, Karnataka, India
来源：
MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 10期
关键词：
Pyran; Thiazolidin-4-one; Piperazine; Anticancer activity; Ehrlich Ascites Carcinoma cells; MolegroVirtual Docker; GABARPL1;
D O I：
10.1007/s00044-013-0478-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel Pyran scaffolds of Thiazolidin-4-one [RA-3(a-d)] and Piperazine [BR (1-4)] were synthesized as potent bi-heterocyclic molecules. All the newly synthesized compounds were confirmed by spectral studies. These synthesized compounds were screened for in vivo anticancer activity. Compounds RA-3a, RA-3c, and BR-3 displayed the highest anticancer activity against Ehrlich Ascites Carcinoma cells and docking study of all the synthesized title compounds was carried out using Molegro Virtual Docker on GABARAPL1 (GABA(A) receptor-associated protein-1 cancer receptor). These studies revealed the importance of Pyranone, Thiazolidnones, and Piperazine nucleus for their anticancer activity.
引用
收藏
页码：4909 / 4919
页数：11
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