Synthesis and antitumor activity of camptothecin-4β-triazolopodophyllotoxin conjugates

被引：8

作者：

Zi, Cheng-Ting ^{[1
,2
,3
]}

Yang, Liu ^{[2
]}

Dong, Fa-Wu ^{[2
]}

Kong, Qing-Hua ^{[2
]}

Ding, Zhong-Tao ^{[3
]}

Zhou, Jun ^{[2
]}

Jiang, Zi-Hua ^{[4
]}

Hu, Jiang-Miao ^{[2
]}

机构：

[1] Yunnan Agr Univ, Coll Sci, Key Lab Pu Er Tea Sci, Minist Educ, Kunming, Yunnan, Peoples R China

[2] Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming, Yunnan, Peoples R China

[3] Yunnan Univ, Sch Chem Sci & Technol, Key Lab Med Chem Nat Resource, Minist Educ, Kunming, Yunnan, Peoples R China

[4] Lakehead Univ, Dept Chem, Thunder Bay, ON, Canada

来源：

NATURAL PRODUCT RESEARCH | 2020年 / 34卷 / 16期

关键词：

antitumor activity; CuAAC reaction; camptothecin; podophyllotixin; DNA CLEAVABLE COMPLEXES; TOPOISOMERASE-II; REPLICATION FORKS; AGENTS; CAMPTOTHECIN; PODOPHYLLOTOXIN; INHIBITORS; CYTOTOXICITY; DERIVATIVES; CONGENERS;

D O I：

10.1080/14786419.2018.1538223

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Two new compounds (9 and 10) having a camptothecin (CPT) analog conjugated to the 4 beta-azido-4-deoxypodophyllotixin analog by untilizing the copper-catalyzed azide-alkyne cycloadditon (CuAAC) reaction, and were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using the MTT (3-(4,5-dimethyl-thiahiazo-2-yl)-2,5-diphenyltetrazolium bromide) assay. Two novel conjugates shown weak cytotoxicity, compound 10 showed highly potent against HL-60 cell line tested, with IC50 value 17.69 +/- 0.19 mu M. This compound suggested its potential as anticancer agents for further development. [GRAPHICS] .

引用

页码：2301 / 2309

页数：9

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