Synthesis and antitumor properties of N1-(hydroxymethyl phenylmethyl) pyrimidine derivatives and their intermediates

被引：5

作者：

Chen, Liying ^{[1
]}

Kode, Nageswara ^{[1
]}

Murthy, Devangachinta ^{[1
]}

Phadtare, Shashikant ^{[1
]}

机构：

[1] Xavier Univ, Coll Pharm, Div Basic Pharmaceut Sci, New Orleans, LA 70125 USA

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2007年 / 4卷 / 04期

关键词：

arylpyrimidines; N1-[(chloromethylphenyl)methyl]pyrimidines; GI(50); antitumor activity;

D O I：

10.2174/157018007784620022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of ortho- meta- and pora-N1-[(chloromethylphenyl)methyl]pyrimidines and N1[(hydroxymethylphenyl)methyl]pyrimidines 4-27 were prepared by the alkylation of various pyrimidine nucleic acid bases with alpha,alpha'-dichloroxylenes followed by acid catalyzed hydrolysis. Compounds 4-27 were evaluated for the cytotoxic activity against a panel NCI-H460 (lung), MCF7 (breast) and SF-268 (CNS) cancer cell lines. The 'active' compounds which reduced growth of cancer cells to ca. 32% or less have been evaluated in the full panel of 60 human cancer cell lines over a 5-log dose range at the National Cancer Institute. Specifically, the ortho-N1-[(chloromethylphenyl)methyl]pyrimidines in this series (5, 6 and 7) have demonstrated growth inhibitory effects (GI(50)) on the leukemia (CCRF-CEM, HL-60, K562, MOLT-4, SR) and other cancer cell lines at 10(-5) to 10(-7) M concentrations.

引用

页码：249 / 256

页数：8

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