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Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities.
Bioorg Med Chem. 2010 May 01; 18(9):3140-6.BM

Abstract

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.

Authors+Show Affiliations

School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20371183

Citation

Miao, Zhenyuan, et al. "Phosphate Ester Derivatives of Homocamptothecin: Synthesis, Solution Stabilities and Antitumor Activities." Bioorganic & Medicinal Chemistry, vol. 18, no. 9, 2010, pp. 3140-6.
Miao Z, Zhang J, You L, et al. Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities. Bioorg Med Chem. 2010;18(9):3140-6.
Miao, Z., Zhang, J., You, L., Wang, J., Sheng, C., Yao, J., Zhang, W., Feng, H., Guo, W., Zhou, L., Liu, W., Zhu, L., Cheng, P., Che, X., Wang, W., Luo, C., Xu, Y., & Dong, G. (2010). Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities. Bioorganic & Medicinal Chemistry, 18(9), 3140-6. https://doi.org/10.1016/j.bmc.2010.03.039
Miao Z, et al. Phosphate Ester Derivatives of Homocamptothecin: Synthesis, Solution Stabilities and Antitumor Activities. Bioorg Med Chem. 2010 May 1;18(9):3140-6. PubMed PMID: 20371183.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities. AU - Miao,Zhenyuan, AU - Zhang,Jing, AU - You,Liang, AU - Wang,Juan, AU - Sheng,Chunquan, AU - Yao,Jiangzhong, AU - Zhang,Wannian, AU - Feng,Hao, AU - Guo,Wei, AU - Zhou,Lei, AU - Liu,Wenfeng, AU - Zhu,Linjian, AU - Cheng,Pengfei, AU - Che,Xiaoying, AU - Wang,Wenya, AU - Luo,Chuan, AU - Xu,Yulan, AU - Dong,Guoqiang, Y1 - 2010/03/20/ PY - 2010/02/10/received PY - 2010/03/15/revised PY - 2010/03/16/accepted PY - 2010/4/8/entrez PY - 2010/4/8/pubmed PY - 2010/9/11/medline SP - 3140 EP - 6 JF - Bioorganic & medicinal chemistry JO - Bioorg. Med. Chem. VL - 18 IS - 9 N2 - 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. SN - 1464-3391 UR - https://www.unboundmedicine.com/medline/citation/20371183/Phosphate_ester_derivatives_of_homocamptothecin:_synthesis_solution_stabilities_and_antitumor_activities_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0968-0896(10)00243-9 DB - PRIME DP - Unbound Medicine ER -