Substituted thiazoles V. Synthesis and antitumor activity of novel thiazolo[2,3-b]quinazoline and pyrido[4,3-d]thiazolo[3,2-a]pyrimidine analogues

被引：105
作者：
Al-Omary, Fatmah A. M. [4 ]
Hassan, Ghada S. [3 ,4 ]
El-Messery, Shahenda M. [2 ]
El-Subbagh, Hussein I. [1 ]
机构：
[1] Future Univ, Fac Pharmaceut Sci & Pharmaceut Ind, Dept Pharmaceut Chem, Cairo 12311, Egypt
[2] Mansoura Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Mansoura, Egypt
[3] Mansoura Univ, Fac Pharm, Dept Med Chem, Mansoura, Egypt
[4] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 47卷
关键词：
Thiazolo[2,3-b]quinazoline and pyrido[4,3-d]thiazolo[3,2-a]pyrimidine; Antitumor activity; BIOLOGICAL EVALUATION; 2,4-DISUBSTITUTED THIAZOLES; THYMIDYLATE SYNTHASE; AGENTS; DERIVATIVES; ANTICANCER; INHIBITORS; 2,6-BIS(ARYLIDENE)CYCLOHEXANONES; CYTOTOXICITY; ANGIOGENESIS;
D O I：
10.1016/j.ejmech.2011.10.023
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of thiazolo[2,3-b]quinazoline (14-23, 26 and 27), and pyrido[4,3-d]thiazolo[3,2-a] pyrimidine (34-43, 45 and 46) analogues were designed and synthesized. The obtained compounds were evaluated for their in-vitro antitumor activity at the National Cancer Institute (NCI) 60 cell lines panel assay. Compounds 22, 38, 40 and 41 showed remarkable broad-spectrum antitumor activity. Compounds 22 and 38 are almost nine fold more active than 5-FU, with GI(50), TGI, and LC50 values of 2.5, >100, >100; and 2.4, 9.1, 36.2 mu M, respectively; while 40 and 41 are almost seven fold more active than 5-FU, with GI(50), TGI, and LC50 values of 2.9, 12.4, 46.6 and 3.0, 16.3, 54.0 mu M, respectively. (C) 2011 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：65 / 72
页数：8
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