Synthesis and antiproliferative activity of 2-(([1,2,4]triazolo[4,3-b]-pyridazin-6-yloxy)methyl)-2,4-dimethyl-3,4-dihydro-2H-benzo[b][1,4]oxazine derivatives

被引：4

作者：

Ilic, Milos ^{[1
]}

Ilas, Janez ^{[1
]}

Liekens, Sandra ^{[2
]}

Matyus, Peter ^{[3
]}

Kikelj, Danijel ^{[1
]}

机构：

[1] Univ Ljubljana, Fac Pharm, Askerceva 7, Ljubljana 1000, Slovenia

[2] Catholic Univ Louvain, Rega Inst Med Res, B-3000 Louvain, Belgium

[3] Semmelweis Univ, Dept Organ Chem, H-1092 Budapest, Hungary

来源：

ARKIVOC | 2011年

关键词：

1,2,4]Triazolo[4,3-b]pyridazine; 2,4-dimethyl-3,4-dihydro-2H-benzo[b][1,4]-oxazine; Mitsunobu reaction; benzamidine; thrombin inhibitor; cell proliferation; ANTITHROMBOTIC COMPOUNDS;

D O I：

10.3998/ark.5550190.0012.a25

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A small library of [1,2,4]triazolo[4,3-b]pyridazin-6-yloxy derivatives 14-17 of N-benzyl-N-(2((4-amidinophenoxy)methyl)-2,4-dimethyl-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)-oxalic acid monoamides 1 was prepared by replacement of benzamidine with a [1,2,4] triazolo[4,3b] pyridazine-6-yl moiety. Thrombin inhibitory and fibrinogen receptor antagonistic activities inherent to benzamidine compounds 1 were lost in the [1,2,4]triazolo[4,3-b]pyridazine derivatives 14-17 which, on the other side, in their ester form (R-2 = Et) inhibited the proliferation of endothelial and tumor cells.

引用

页码：309 / 322

页数：14

共 16 条

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