Synthesis of Dihydropyrimidin-2-one/thione Library and Cytotoxic Activity against the Human U138-MG and Rat C6 Glioma Cell Lines

被引：57

作者：

Canto, Romulo F. S. ^{[2
]}

Bernardi, Andressa ^{[3
]}

Battastini, Ana Maria O. ^{[3
]}

Russowsky, Dennis ^{[1
]}

Eifler-Lima, Vera Lucia ^{[2
]}

机构：

[1] Univ Fed Rio Grande do Sul, Inst Quim, BR-91501970 Porto Alegre, RS, Brazil

[2] Univ Fed Rio Grande do Sul, Lab Sintese Organ Med LaSOM, Programa Posgrad Ciencias Farmaceut, BR-9061000 Porto Alegre, RS, Brazil

[3] Univ Fed Rio Grande do Sul, Inst Ciencias Basic Saude, BR-90035003 Porto Alegre, RS, Brazil

来源：

JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY | 2011年 / 22卷 / 07期

关键词：

dihydropyrimidin-2(1H)-ones; Biginelli reaction; triethylorthoformate; TEOF; monastrol; cancer; glioma; ONE-POT SYNTHESIS; CATALYZED BIGINELLI REACTION; SOLVENT-FREE BIGINELLI; SOLID-PHASE SYNTHESIS; REUSABLE CATALYST; ANTIPROLIFERATIVE ACTIVITY; EFFICIENT CATALYST; FLUOROUS SYNTHESIS; IMPROVED PROTOCOL; SMALL-MOLECULE;

D O I：

10.1590/S0103-50532011000700025

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Two series of 4-aryl-3,4-dihydropyrimidin-2(1H)-(thio) ones including monastrol (1a), have been synthesized by an environment-friendly methodology based on the combined use of citric acid or oxalic acid and TEOF (triethylorthoformate). The library was evaluated as inhibitor of cell proliferation on two glioma cell lines (human-U138-MG and Rat-C6). The compounds derived from thiourea 1f and 1d were more cytotoxic than monastrol. The compound derived from urea 2d showed the highest cytotoxic activity among the analyzed compounds.

引用

页码：1379 / 1388

页数：10

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