Novel 5′-Norcarbocyclic Derivatives of Bicyclic Pyrrolo- and Furano[2,3-d]Pyrimidine Nucleosides

被引：7

作者：

Klimenko, Anna A. ^{[1
]}

Matyugina, Elena S. ^{[1
]}

Logashenko, Evgeniya B. ^{[2
]}

Solyev, Pavel N. ^{[1
]}

Zenkova, Marina A. ^{[2
]}

Kochetkov, Sergey N. ^{[1
]}

Khandazhinskaya, Anastasia L. ^{[1
]}

机构：

[1] Russian Acad Sci, Engelhardt Inst Mol Biol, 32 Vavilov St, Moscow 119991, Russia

[2] Russian Acad Sci, Inst Chem Biol & Fundamental Med, Siberian Branch, 8 Lavrentiev Ave, Novosibirsk 630090, Russia

来源：

MOLECULES | 2018年 / 23卷 / 10期

基金：

俄罗斯基础研究基金会;

关键词：

5 '-norcarbocyclic nucleoside analogues; antiproliferative properties; structure-activity relationship; BIOLOGICAL EVALUATION; ANALOGS; INHIBITORS; POTENT; VZV;

D O I：

10.3390/molecules23102654

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Here we report the synthesis and biological activity of new 5'-norcarbocyclic derivatives of bicyclic pyrrolo-and furano[2,3-d]pyrimidines with different substituents in the heterocyclic ring. Lead compound 3i, containing 6-pentylphenyl substituent, displays inhibitory activity with respect to a number of tumor cells with a moderate selectivity index value. Compound 3i induces cell death by the apoptosis pathway with the dissipation of mitochondrial potential.

引用

页数：12