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Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.
Bioorg Med Chem Lett. 2014 Mar 15; 24(6):1597-9.BM

Abstract

In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibitory effects on topoisomerase I. All of the new compounds showed potent inhibition of human tumor cell growth, among which compound 10a showed higher cytotoxic activity than that of SN-38. Furthermore, this series of compounds retained or enhanced Topo I inhibition.

Authors+Show Affiliations

Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Shanghai 201203, PR China.State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Shanghai 201203, PR China.State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Shanghai 201203, PR China. Electronic address: ychen@jding.dhs.org.Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China. Electronic address: qqhuang@sat.ecnu.edu.cn.

Pub Type(s)

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

Language

eng

PubMed ID

24529870

Citation

Wang, Lei, et al. "Suzuki Coupling Based Synthesis and in Vitro Cytotoxic Evaluation of 7-heteroaryl-substituted Camptothecin Analogs." Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 6, 2014, pp. 1597-9.
Wang L, Huang Y, Zhang J, et al. Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs. Bioorg Med Chem Lett. 2014;24(6):1597-9.
Wang, L., Huang, Y., Zhang, J., Tong, L., Chen, Y., Lu, W., & Huang, Q. (2014). Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs. Bioorganic & Medicinal Chemistry Letters, 24(6), 1597-9. https://doi.org/10.1016/j.bmcl.2014.01.049
Wang L, et al. Suzuki Coupling Based Synthesis and in Vitro Cytotoxic Evaluation of 7-heteroaryl-substituted Camptothecin Analogs. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1597-9. PubMed PMID: 24529870.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs. AU - Wang,Lei, AU - Huang,Ying, AU - Zhang,Jie, AU - Tong,Linjiang, AU - Chen,Yi, AU - Lu,Wei, AU - Huang,Qingqing, Y1 - 2014/01/29/ PY - 2013/12/06/received PY - 2014/01/15/revised PY - 2014/01/20/accepted PY - 2014/2/18/entrez PY - 2014/2/18/pubmed PY - 2014/11/5/medline KW - Antitumor KW - C-7-heteroaryl-substituted camptothecin KW - Camptothecin KW - Suzuki coupling SP - 1597 EP - 9 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 24 IS - 6 N2 - In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibitory effects on topoisomerase I. All of the new compounds showed potent inhibition of human tumor cell growth, among which compound 10a showed higher cytotoxic activity than that of SN-38. Furthermore, this series of compounds retained or enhanced Topo I inhibition. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/24529870/Suzuki_coupling_based_synthesis_and_in_vitro_cytotoxic_evaluation_of_7_heteroaryl_substituted_camptothecin_analogs_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(14)00079-1 DB - PRIME DP - Unbound Medicine ER -