Synthesis and anticancer activity of some 1,5-diaryl-3-(3,4,5-trihydroxyphenyl)-1H-pyrazolo[4,3-e][1,2,4]triazines

被引：17

作者：

Gucky, Tomas ^{[1
,2
]}

Reznickova, Eva ^{[1
,2
]}

Dzubak, Petr ^{[3
,4
]}

Hajduch, Marian ^{[3
,4
]}

Krystof, Vladimir ^{[1
,2
]}

机构：

[1] Palacky Univ, Lab Growth Regulators, Fac Sci, Olomouc 78371, Czech Republic

[2] ASCR, Inst Expt Bot, Olomouc 78371, Czech Republic

[3] Palacky Univ, Expt Med Lab, Inst Mol & Translat Med, Fac Med & Dent, Olomouc 78371, Czech Republic

[4] Fac Hosp Olomouc, Olomouc, Czech Republic

来源：

MONATSHEFTE FUR CHEMIE | 2010年 / 141卷 / 06期

关键词：

Pyrazolo[4,3-e][1,2,4]triazine; Anticancer; Cyclin-dependent kinase; Inhibitor; Caspase; Apoptosis; DEPENDENT KINASE INHIBITOR; MULTIPLE-MYELOMA CELLS; DOWN-REGULATION; PSEUDOMONAS-FLUORESCENS; SELICICLIB CYC202; R-ROSCOVITINE; MCL-1; DERIVATIVES; MODULATORS; POTENT;

D O I：

10.1007/s00706-010-0314-4

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The deregulation of cell cycle components in cancer cells has provided a rationale for the development of small molecule inhibitors of cyclin-dependent kinases as novel anticancer drugs. A series of 1,5-diaryl-3-(3,4,5-trihydroxyphenyl)-1H-pyrazolo[4,3-e][1,2,4]triazines was synthesized and their kinase inhibitory activity and cytotoxicity against several cancer cell lines has been evaluated. Some of the compounds of the series exhibited induction of caspase-dependent cell death and inhibition of cyclin-dependent kinase 2 (CDK2).

引用

收藏

页码：709 / 714

页数：6

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