7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation |
| |
| Authors: | Mingzong Li Wei Jin Chen Jiang Chao Zheng Weidong Tang Tianpa You Liguang Lou |
| |
| Institution: | 1. Department of Chemistry, University of Science & Technology of China, Hefei, Anhui 230026, PR China;2. Chinese Acad. Sci., Shanghai Inst. Mat. Med., 555 Zuchongzhi Rd, Shanghai 201203, PR China;3. Department of Basic Sciences, China Pharmaceutical University, Nanjing, Jiangsu 210000, PR China |
| |
| Abstract: | A series of 7-cycloalkylcamptothecin derivatives were synthesized from camptothecin with two methods. Their biological activities in vitro were evaluated with sulforhodamine-B (SRB) method on four types of human tumor cell lines A549/ATCC, HT29, NCI-H460 and HL60. Most of these camptothecin analogues show higher antitumor activity than the reference compounds SN-38 and Topotecan, with the IC50 values low to nM level. Structure–activity relationship studies of these compounds mostly match the conclusion we achieved before from quantitative structure–activity relationship (QSAR) research. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
