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Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors.
Eur J Med Chem. 2011 Jun; 46(6):2408-14.EJ

Abstract

A series of novel 7-acyl derivatives of homocamptothecin (hCPT) were designed and synthesized with the purpose to improve antitumor activity of hCPT, via Minisci free-radical reaction from 10-methoxyhomocamptothecin. All the compounds were evaluated for in vitro cytotoxicity against three cancer cell lines (A549, MDA-MB-435 and HCT116). For MDA-MB-435 cell line, compounds, 6a, 6b, 6k and all of 7-alkylcabonyl homocamptothecin derivatives showed higher in vitro inhibitory activities than topotecan (TPT). Furthermore, compounds 6d, 6e, and 6k showed highly potent inhibitory activities with the IC50 values from less than 1 nM to 2.2 nM. In Topoisomerase I (Topo I)-induced DNA cleavage assay, compounds 6a, 6d, and 6k, as compared to CPT, revealed higher Topo I inhibitory activity.

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 available

Pub Type(s)

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

Language

eng

PubMed ID

21463912

Citation

Liu, Wenfeng, et al. "Synthesis and Biological Evaluation of Novel 7-acyl Homocamptothecins as Topoisomerase I Inhibitors." European Journal of Medicinal Chemistry, vol. 46, no. 6, 2011, pp. 2408-14.
Liu W, Zhu L, Guo W, et al. Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors. Eur J Med Chem. 2011;46(6):2408-14.
Liu, W., Zhu, L., Guo, W., Zhuang, C., Zhang, Y., Sheng, C., Cheng, P., Yao, J., Wang, W., Dong, G., Wang, S., Miao, Z., & Zhang, W. (2011). Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors. European Journal of Medicinal Chemistry, 46(6), 2408-14. https://doi.org/10.1016/j.ejmech.2011.03.024
Liu W, et al. Synthesis and Biological Evaluation of Novel 7-acyl Homocamptothecins as Topoisomerase I Inhibitors. Eur J Med Chem. 2011;46(6):2408-14. PubMed PMID: 21463912.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors. AU - Liu,Wenfeng, AU - Zhu,Lingjian, AU - Guo,Wei, AU - Zhuang,Chunlin, AU - Zhang,Yongqiang, AU - Sheng,Chunquan, AU - Cheng,Pengfei, AU - Yao,Jianzhong, AU - Wang,Wenya, AU - Dong,Guoqiang, AU - Wang,Shengzheng, AU - Miao,Zhenyuan, AU - Zhang,Wannian, Y1 - 2011/03/23/ PY - 2011/01/11/received PY - 2011/03/07/revised PY - 2011/03/13/accepted PY - 2011/4/6/entrez PY - 2011/4/6/pubmed PY - 2011/9/13/medline SP - 2408 EP - 14 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 46 IS - 6 N2 - A series of novel 7-acyl derivatives of homocamptothecin (hCPT) were designed and synthesized with the purpose to improve antitumor activity of hCPT, via Minisci free-radical reaction from 10-methoxyhomocamptothecin. All the compounds were evaluated for in vitro cytotoxicity against three cancer cell lines (A549, MDA-MB-435 and HCT116). For MDA-MB-435 cell line, compounds, 6a, 6b, 6k and all of 7-alkylcabonyl homocamptothecin derivatives showed higher in vitro inhibitory activities than topotecan (TPT). Furthermore, compounds 6d, 6e, and 6k showed highly potent inhibitory activities with the IC50 values from less than 1 nM to 2.2 nM. In Topoisomerase I (Topo I)-induced DNA cleavage assay, compounds 6a, 6d, and 6k, as compared to CPT, revealed higher Topo I inhibitory activity. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/21463912/Synthesis_and_biological_evaluation_of_novel_7_acyl_homocamptothecins_as_Topoisomerase_I_inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(11)00238-8 DB - PRIME DP - Unbound Medicine ER -