Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities
| Autor: | Guoqiang Dong, Lei Zhou, Xiaoying Che, Jing Zhang, Wenfeng Liu, Wei Guo, Pengfei Cheng, Hao Feng, Juan Wang, Zhenyuan Miao, Chunquan Sheng, Wenya Wang, Chuan Luo, Jiangzhong Yao, Wannian Zhang, Yulan Xu, Liang You, Lin-Jian Zhu |
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| Rok vydání: | 2010 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Topoisomerase-I Inhibitor Biochemistry Chemical synthesis Phosphates Inhibitory Concentration 50 Structure-Activity Relationship Drug Stability In vivo Cell Line Tumor Drug Discovery Humans Cytotoxicity Molecular Biology Cell Proliferation chemistry.chemical_classification biology Molecular Structure Topoisomerase Organic Chemistry Esters Hydrogen-Ion Concentration In vitro Pharmaceutical Solutions Enzyme chemistry Drug Design biology.protein Molecular Medicine Camptothecin Drug Screening Assays Antitumor Lactone |
| Zdroj: | Bioorganicmedicinal chemistry. 18(9) |
| ISSN: | 1464-3391 |
| Popis: | Homocamptothecins (hCPTs) represents a new promising class of topoisomerase I inhibitors with enhanced stability and superior antitumor activity. Some phosphodiesters and phosphotriesters homocamptothecin derivatives were designed and synthesized based on our previous synthetic route. The cytotoxicity in vitro on three cancer cell lines and antitumor activity in vivo, and inhibitory properties of topoisomerase I of these derivatives were evaluated. Among them compounds 24e and 24f exhibited higher cytotoxic activity than IRT and the former exhibited the best antitumor activity in vivo and solution stability both at pH 7.4 and pH 3.0. |
| Databáze: | OpenAIRE |
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