Synthesis and biological evaluation of a cyclic ether fluorinated noscapine analog

被引：47

作者：

Aneja, Ritu ^{[1
]}

Vangapandu, Surya N. ^{[1
]}

Joshi, Harish C. ^{[1
]}

机构：

[1] Emory Univ, Sch Med, Dept Cell Biol, Lab Drug Discovery & Res, Atlanta, GA 30322 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 24期

关键词：

noscapine; fluorination; cyclic ethers; anticancer; PACLITAXEL RESISTANCE; OVARIAN-CANCER; AGENT; CELLS; APOPTOSIS; DERIVATIVES; PROGRESSION; EM012;

D O I：

10.1016/j.bmc.2006.09.012

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：

We present here a novel semi-synthetic cyclic ether fluorinated noscapine analog (CEFNA) that shows potent antiproliferative and anticancer activity in both hormone-responsive (MCF-7) and hormone non-responsive (MDA-MB-231) breast cancer cells. Interestingly, it is also effective against MCF-7/Adr, an adriamycin-resistant variant of MCF-7 cells. Immunofluorescence experiments showed numerous micronuclei, indicative of apoptotic cell death triggered by this novel analog. Mechanistically, CEFNA exerts a strong antimitotic effect as revealed by cell-cycle studies that show a dose-dependent increase in G2/M population preceding a rising sub-G1 population, suggesting apoptosis. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：8352 / 8358

页数：7

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