Design and synthesis of C35-fluorinated solamins and their growth inhibitory activities against human cancer cell lines

被引：14

作者：

Kojima, Naoto ^{[1
]}

Suga, Yuki ^{[1
]}

Hayashi, Hiromi ^{[1
]}

Yamori, Takao ^{[2
]}

Yoshimitsu, Takehiko ^{[1
]}

Tanaka, Tetsuaki ^{[1
]}

机构：

[1] Osaka Univ, Grad Sch Pharmaceut Sci, Suita, Osaka 5650871, Japan

[2] Japanese Fdn Canc Res, Ctr Canc Chemotherapy, Koto Ku, Tokyo 1358550, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 19期

关键词：

Annonaceous acetogenin; Structure-activity relationship; Antitumor agent; Fluorinated analogue; Chemical synthesis; ANNONACEOUS ACETOGENINS; CONVERGENT SYNTHESIS; MONOTETRAHYDROFURAN-RING; SYSTEMATIC SYNTHESIS; 3-KINASE INHIBITOR; ANTITUMOR-ACTIVITY; CONCISE SYNTHESIS; ANALOGS; STEREODIVERGENT; CORES;

D O I：

10.1016/j.bmcl.2011.08.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The convergent synthesis of C35-fluorinated analogues of solamin, a mono-THF Annonaceous acetogenin, has been achieved by the Sonogashira coupling of the THF ring fragment and the fluorinated gamma-lactone fragment. It was revealed that the number of fluorine atoms on the gamma-lactone moiety affects the growth inhibitory activities against human cancer cell lines. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：5745 / 5749

页数：5

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