Synthesis and biotests of 2-aryl-5-arylmethylidene-substituted 1,3-oxazol-5(4H)-ones and N-methyl-3,5-dihydro-4H-imidazol-4-ones as combretastatin A-4 analogs

被引：5

作者：

Barskaia, E. S. ^{[1
]}

Beloglazkina, A. A. ^{[1
]}

Wobith, B. ^{[2
]}

Zefirov, N. A. ^{[1
]}

Majouga, A. G. ^{[1
]}

Beloglazkina, E. K. ^{[1
]}

Zyk, N. V. ^{[1
]}

Kuznetsov, S. A. ^{[2
]}

Zefirova, O. N. ^{[1
,3
]}

机构：

[1] Moscow MV Lomonosov State Univ, Dept Chem, Build 3,1 Leninskie Gory, Moscow 119991, Russia

[2] Univ Rostock, Inst Biol Sci, D-18106 Rostock, Germany

[3] Russian Acad Sci, Inst Physiol Act Cpds, 1 Severnyi Pr D, Chernogolovka 142432, Moscow Region, Russia

来源：

RUSSIAN CHEMICAL BULLETIN | 2015年 / 64卷 / 07期

基金：

俄罗斯基础研究基金会;

关键词：

combretastatin analogs; oxazolones; imidazolones; colchicine domain; tubulin; cytotoxicity; TUBULIN; DESIGN; SITE;

D O I：

10.1007/s11172-015-1041-0

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of 2-aryl-5-arylmethylidene-1,3-oxazol-5(4H)-ones and 2-aryl-5-arylmethylidene-N-methyl-3,5-dihydro-4H-imidazol-4-ones was synthesized as structural analogs of combret-astatin A-4 (a compound possessing antitumor activity). (5Z)-5-[(4-Methoxyphenyl)methyl-idene]-3-methyl-2-(4-methylphenyl)-3,5-dihydro-4H-imidazol-4-one was found to exhibit the highest cytotoxicity against cells of human A549 lung carcinoma line (EC50 = 6 +/- 0.8 mu mol L-1).

引用

页码：1560 / 1563

页数：4

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