SYNTHESIS AND ANTITUMOR PROPERTIES OF NEW 2,4-DICHLOROPHENOXY ETHERS

被引：3

作者：

Abdel-Wahab, B. F. ^{[1
]}

Farghaly, M. ^{[1
]}

Badria, F. A. ^{[2
]}

机构：

[1] Natl Res Ctr, Appl Organ Chem Dept, Giza, Egypt

[2] Mansoura Univ, Fac Pharm, Dept Pharmacognosy, Mansoura 35516, Egypt

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2011年 / 45卷 / 01期

关键词：

2,4-dichlorophenoxyacetic acid; imidazo[2,1-b][1,3,4]thiadiazoles; pyrazoles; hydrazonoyl chlorides; thiosemicarbazides; 1,3,4-thiadiazoles; antitumor activity; ANTIMICROBIAL ACTIVITY; DERIVATIVES; PYRAZOLINES;

D O I：

10.1007/s11094-011-0555-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new compounds incorporating 2,4-dichlorophenoxy nucleus have been synthesized. Reaction of 2,4-dichlorophenoxyacetic acid with thiosemicarbazide in the presence of phosphoryl chloride followed by treatment with phenacylbromides led to the formation of imidazo[2,1-b][1,3,4] thiadiazoles (3). Bischlorophenoxyallyl hydrazides (4) reacted with some of alkenes, azo dyes, aldehydes, and hydrazonoyl chlorides to produce pyrazoles, Schiff bases, and bis-diazo compounds, respectively. 1,3,4-Thiadiazole (10) was obtained by reaction of dichlorophenoxyallyl hydrazides (4b) with carbon disulphide followed by hydrazonoyl chlorides. All compounds were tested for their preliminarily antitumor activity on transplantable murine tumor cell line [Ehrlich ascites carcinoma (EAC)]. Compound 2-{2-[2-(2,4-dichlorophenoxy) acetyl]hydrazono}-N'-(4-fluorophenyl) propanehydrazonoyl chloride (8c) has remarkably decreased the viable EAC cell count as indicated by Trypan Blue dye exclusion test (3%) in comparison to the well known antitumor agent 5-FU (0%).

引用

页码：30 / 35

页数：6

共 28 条

[1] Synthesis and antimicrobial evaluation of 1-(benzofuran-2-yl)-4-nitro-3-arylbutan-1-ones and 3-(benzofuran-2-yl)-4,5-dihydro-5-aryl-1-[4-(aryl)-1, 3-thiazol-2-yl]-1H-pyrazoles [J].