Synthesis and antitumor activity of camptothecin- 4β-triazolopodophyllotoxin conjugates. Issue 16 (17th August 2020)

• Record Type: Journal Article
• Authors: Zi, Cheng-Ting; Yang, Liu; Dong, Fa-Wu; Kong, Qing-Hua; Ding, Zhong-Tao; Zhou, Jun; Jiang, Zi-Hua; Hu, Jiang-Miao
• Is Part Of: Natural product research. Volume 34:Issue 16(2020)
• Page Start: 2301
• Page End: 2309
• Publication Date: 2020-08-17
• Subjects: antitumor activity -- CuAAC reaction -- camptothecin -- podophyllotixin; Natural products -- Periodicals; Natural products -- Research -- Periodicals; Biological Factors -- Periodicals; Biological Products -- Periodicals; 547
• DOI: 10.1080/14786419.2018.1538223
• Languages: English
• ISSNs: 1478-6419

Abstract

Abstract: Two new compounds (9 and 10 ) having a camptothecin (CPT) analog conjugated to the 4β-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 μM. This compound suggested its potential as anticancer agents for further development.