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Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin.
Bioorg Med Chem Lett. 2008 Dec 15; 18(24):6441-3.BM

Abstract

A series of E-ring gamma-lactone camptothecin derivatives were synthesized by semi-synthesis via a three-step domino reaction. Their biological activity was evaluated on two types of human tumor cell lines A549 and HT-29 with sulforhodamine-B (SRB) method. The antitumor activity of these compounds was lower than SN-38, only compound 12c was found to be close to the activity of Topotecan. The structure-activity relationship (SAR) of these analogs was studied and discussed.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Li M
Department of Chemistry, University of Science & Technology of China, Hefei, Anhui 230026, PR China.
Tang W
No affiliation info available
Zeng F
No affiliation info available
Lou L
No affiliation info available
You T
No affiliation info available

MeSH

Antineoplastic Agents, PhytogenicCamptothecaCamptothecinCell Line, TumorDNA Topoisomerases, Type IDrug DesignDrug Screening Assays, AntitumorHumansInhibitory Concentration 50IrinotecanLactonesModels, ChemicalMolecular StructureSolubilityStructure-Activity Relationship

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18986807

Citation

Li, Mingzong, et al. "Semi-synthesis and Biological Activity of Gamma-lactones Analogs of Camptothecin." Bioorganic & Medicinal Chemistry Letters, vol. 18, no. 24, 2008, pp. 6441-3.
Li M, Tang W, Zeng F, et al. Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin. Bioorg Med Chem Lett. 2008;18(24):6441-3.
Li, M., Tang, W., Zeng, F., Lou, L., & You, T. (2008). Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin. Bioorganic & Medicinal Chemistry Letters, 18(24), 6441-3. https://doi.org/10.1016/j.bmcl.2008.10.074
Li M, et al. Semi-synthesis and Biological Activity of Gamma-lactones Analogs of Camptothecin. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6441-3. PubMed PMID: 18986807.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin. AU - Li,Mingzong, AU - Tang,Weidong, AU - Zeng,Fuxing, AU - Lou,Liguang, AU - You,Tianpa, Y1 - 2008/10/19/ PY - 2008/08/31/received PY - 2008/10/13/revised PY - 2008/10/16/accepted PY - 2008/11/7/pubmed PY - 2009/4/30/medline PY - 2008/11/7/entrez SP - 6441 EP - 3 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 18 IS - 24 N2 - A series of E-ring gamma-lactone camptothecin derivatives were synthesized by semi-synthesis via a three-step domino reaction. Their biological activity was evaluated on two types of human tumor cell lines A549 and HT-29 with sulforhodamine-B (SRB) method. The antitumor activity of these compounds was lower than SN-38, only compound 12c was found to be close to the activity of Topotecan. The structure-activity relationship (SAR) of these analogs was studied and discussed. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/18986807/Semi_synthesis_and_biological_activity_of_gamma_lactones_analogs_of_camptothecin_ DB - PRIME DP - Unbound Medicine ER -