Novel N-(phosphonomethyl) glycine derivatives:: Design, characterization and biological activity

被引:39
作者
Naydenova, Emilia D. [2 ]
Todorov, Petar T. [2 ]
Topashka-Ancheva, Margarita N. [3 ]
Momekov, Georgi Ts. [4 ]
Yordanova, Tsvetelina Z. [3 ]
Konstantinov, Spiro M. [4 ]
Troev, Kolio D. [1 ]
机构
[1] Bulgarian Acad Sci, Inst Polymers, BU-1113 Sofia, Bulgaria
[2] Univ Chem Technol & Met, Dept Organ Chem, BU-1756 Sofia, Bulgaria
[3] Bulgarian Acad Sci, Inst Zool, Sofia 1000, Bulgaria
[4] Med Univ Sofia, Lab Expt Chemotherapy, Dept Pharmacol Pharmacotherapy & Toxicol, Fac Pharm, Sofia 1000, Bulgaria
关键词
aminophosphonic acids; N-(phosphonomethyl) glycine derivatives; chromosome aberrations; cell proliferation; clastogenic effects; cytotoxic activity;
D O I
10.1016/j.ejmech.2007.08.010
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of C alpha,alpha-disubstituted cyclic derivatives of N-(phosphonomethyl) glycine have been synthesized and characterized. They exhibited moderate clastogenicity, low antiproliferative activity on mice bone marrow cells and well expressed cytotoxicity against human tumor cell lines. The 8- and 12-membered cyclic analogs proved superior to the remaining compounds and were found to trigger apoptotic cell death in DOHH-2 cells. The latter compound caused 50% inhibition of the viability of hemobastose-derived cell lines at concentrations ranging from 20 to 67 mu M. (c) 2007 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:1199 / 1205
页数:7
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