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Synthesis and biological evaluation of new homocamptothecin analogs.
Eur J Med Chem. 2012 Aug; 54:281-6.EJ

Abstract

In order to increase the stability of E-ring of homocamptothecins, the electron-withdrawing group -OH or -OAc was induced to α position of ring-E lactone. Ten new homocamptothecin analogs were synthesized. Most compounds showed potent in vitro anticancer activity and potent Topo I inhibition, which was equal or superior to that of CPT, SN-38 and 10-HCPT. The stability studies of this series also displayed significant improvement of the stability.

Authors+Show Affiliations

Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, 3663 North Zhongshan Road, East China Normal University, Shanghai 200062, China.No 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

22647222

Citation

Luo, Yu, et al. "Synthesis and Biological Evaluation of New Homocamptothecin Analogs." European Journal of Medicinal Chemistry, vol. 54, 2012, pp. 281-6.
Luo Y, Yu S, Tong L, et al. Synthesis and biological evaluation of new homocamptothecin analogs. Eur J Med Chem. 2012;54:281-6.
Luo, Y., Yu, S., Tong, L., Huang, Q., Lu, W., & Chen, Y. (2012). Synthesis and biological evaluation of new homocamptothecin analogs. European Journal of Medicinal Chemistry, 54, 281-6. https://doi.org/10.1016/j.ejmech.2012.05.002
Luo Y, et al. Synthesis and Biological Evaluation of New Homocamptothecin Analogs. Eur J Med Chem. 2012;54:281-6. PubMed PMID: 22647222.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and biological evaluation of new homocamptothecin analogs. AU - Luo,Yu, AU - Yu,Shanbao, AU - Tong,Linjiang, AU - Huang,Qingqing, AU - Lu,Wei, AU - Chen,Yi, Y1 - 2012/05/15/ PY - 2012/01/13/received PY - 2012/03/20/revised PY - 2012/05/03/accepted PY - 2012/6/1/entrez PY - 2012/6/1/pubmed PY - 2012/12/12/medline SP - 281 EP - 6 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 54 N2 - In order to increase the stability of E-ring of homocamptothecins, the electron-withdrawing group -OH or -OAc was induced to α position of ring-E lactone. Ten new homocamptothecin analogs were synthesized. Most compounds showed potent in vitro anticancer activity and potent Topo I inhibition, which was equal or superior to that of CPT, SN-38 and 10-HCPT. The stability studies of this series also displayed significant improvement of the stability. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/22647222/Synthesis_and_biological_evaluation_of_new_homocamptothecin_analogs_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(12)00299-1 DB - PRIME DP - Unbound Medicine ER -