Anti-breast cancer activity of some novel 1,2-dihydropyridine, thiophene and thiazole derivatives

被引：154

作者：

Al-Said, Mansour S. ^{[1
]}

Bashandy, Mahmoud S. ^{[2
]}

Al-Qasoumi, Saleh I. ^{[3
]}

Ghorab, Mostafa M. ^{[1
]}

机构：

[1] King Saud Univ, Coll Pharm, MAPPRC, Riyadh 11451, Saudi Arabia

[2] Al Azhar Univ, Fac Sci, Dept Chem, Cairo, Egypt

[3] King Saud Univ, Coll Pharm, Dept Pharmacognosy, Riyadh 11451, Saudi Arabia

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 01期

关键词：

Sulfones; 1,2-Dihydropyridines; Thiophenes; Thiazole; Anticancer activity; ANTICANCER;

D O I：

10.1016/j.ejmech.2010.10.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A variety of novel 1,2-dihydropyridines 10-17, thiophenes 18-21 and thiazole 22 having a biologically active sulfone moiety were obtained via the reaction of 2-cyano-N'-[1-(4-(piperidin-1-ylsulfonyl) phenyl) ethylidene] acetohydrazide 3 with a variety of reagents. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, H-1 NMR, C-13 NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in-vitro anticancer activity against human breast cancer cell line (MCF7). Compounds 15 and 11 with IC50 values (20.6, 25.5 mu M) exhibited better activity than Doxorubicin as a reference drug with IC50 value (32.02 mu M), while compound 14 is nearly as active as Doxorubicin as positive control. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：137 / 141

页数：5

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