Synthesis and antitumor activity of biotinylated camptothecin derivatives as potent cytotoxic agents. Issue 2 (15th January 2019)

• Record Type: Journal Article
• Authors: Zi, Cheng-Ting; Yang, Liu; Xu, Feng-Qing; Dong, Fa-Wu; Ma, Rui-Jing; Li, Yan; Zhou, Jun; Ding, Zhong-Tao; Jiang, Zi-Hua; Hu, Jiang-Miao
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 2(2019)
• Page Start: 234
• Page End: 237
• Publication Date: 2019-01-15
• Subjects: Biotinylated camptothecin derivatives -- Anticancer activity -- Synthesis -- Click chemistry -- Structure-activity relationships (SARs); Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.11.049
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Highlights: A series of novel biotinylated camptothecin derivatives were synthesized. The key of the synthesis was achieved byClick chemistry. All of the new derivatives were tested for cytotoxicities. Biotinylated camptothecin derivatives were discussed for exploring novel anticancer agents. Abstract: A series of biotinylated camptothecin derivatives were designed and synthesized. The key to the synthesis was achieved by employing an esterification reaction and click chemistry. All of the new derivatives were tested for cytotoxicity against five human tumor cell lines, including HL-60, SMMC-7721, A-549, MCF-7, and SW480 with IC50 values ranging from 0.13 to 21.53 μM. Most of the derivatives exhibited potent cytotoxicity, especially compound17 (IC50 = 0.13–3.31 μM) and compound18 (IC50 = 0.23–1.48 μM), which exhibited the highest potencies. The structure-activity relationships (SARs) of the biotinylated camptothecin derivatives were discussed for exploring novel anticancer agents.