One pot synthesis of thiazolodihydropyrimidinones and evaluation of their anticancer activity

被引：113

作者：

Holla, BS ^{[1
]}

Rao, BS

Sarojini, BK

Akberali, PM

机构：

[1] Mangalore Univ, Dept Postgrad Studies & Res Chem, Mangalagangothri 574199, India

[2] Strides Arco Labs, New Mangalore 575011, Karnataka, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 39卷 / 09期

关键词：

MCR; three component reaction; thiazolodihydropyrimidinones; arylfurfural; 5-nitrofurfuraldiacetate; anticancer activity;

D O I：

10.1016/j.ejmech.2004.06.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-(5-Arylfur-furylidene/5-nitrofurfurylidene)-5-aryl-7-(2,4-dichloro-5-fluorophenyl)-5H-thiazolo[2,3-b]-pyrimidin-2(1H)-ones 5 and 6 are synthesized by a novel three component reaction of 4,6-diarylpyrimidino-2(1H)-thiones 4, monochloroacetic acid, arylfurfuraldehydes and 5-nitro-2-furfuraldenediacetate, respectively. The newly synthesized compounds are characterized by elemental analysis, IR, H-1 NMR and mass spectral studies. These compounds exhibited in vitro antitumour activity with moderate to excellent growth inhibition against a panel of 60 cell lines of leukemia, non-small cell lung cancer melanoma, ovarian cancer, prostate cancer and breast cancer. GRAPHICS (C) 2004 Elsevier SAS. All rights reserved.

引用

页码：777 / 783

页数：7

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