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Camptothecin-7-yl-methanthiole: semisynthesis and biological evaluation.
ChemMedChem. 2012 Dec; 7(12):2134-43.C

Abstract

The introduction of a methylenthiol group at position 7 of camptothecin was carried out in four steps. This preparation also yielded the corresponding disulfide, which behaves as a prodrug due to its reactivity with glutathione. Assessment of their antiproliferative activities, investigations of their mechanism of action, and molecular modeling analysis indicated that the 7-modified camptothecin derivatives described herein maintain the biological activity and drug-target interactions of the parent compound.

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Authors+Show Affiliations

Christodoulou MS
Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy.
Zunino F
No affiliation info available
Zuco V
No affiliation info available
Borrelli S
No affiliation info available
Comi D
No affiliation info available
Fontana G
No affiliation info available
Martinelli M
No affiliation info available
Lorens JB
No affiliation info available
Evensen L
No affiliation info available
Sironi M
No affiliation info available
Pieraccini S
No affiliation info available
Dalla Via L
No affiliation info available
Gia OM
No affiliation info available
Passarella D
No affiliation info available

MeSH

Antineoplastic Agents, PhytogenicCamptothecinCell Line, TumorCell ProliferationCell SurvivalDNA TopoisomerasesGlutathioneHumansModels, MolecularNeoplasmsProdrugsTopoisomerase I Inhibitors

Pub Type(s)

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

Language

eng

PubMed ID

23086693

Citation

Christodoulou, Michael S., et al. "Camptothecin-7-yl-methanthiole: Semisynthesis and Biological Evaluation." ChemMedChem, vol. 7, no. 12, 2012, pp. 2134-43.
Christodoulou MS, Zunino F, Zuco V, et al. Camptothecin-7-yl-methanthiole: semisynthesis and biological evaluation. ChemMedChem. 2012;7(12):2134-43.
Christodoulou, M. S., Zunino, F., Zuco, V., Borrelli, S., Comi, D., Fontana, G., Martinelli, M., Lorens, J. B., Evensen, L., Sironi, M., Pieraccini, S., Dalla Via, L., Gia, O. M., & Passarella, D. (2012). Camptothecin-7-yl-methanthiole: semisynthesis and biological evaluation. ChemMedChem, 7(12), 2134-43. https://doi.org/10.1002/cmdc.201200322
Christodoulou MS, et al. Camptothecin-7-yl-methanthiole: Semisynthesis and Biological Evaluation. ChemMedChem. 2012;7(12):2134-43. PubMed PMID: 23086693.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Camptothecin-7-yl-methanthiole: semisynthesis and biological evaluation. AU - Christodoulou,Michael S, AU - Zunino,Franco, AU - Zuco,Valentina, AU - Borrelli,Stella, AU - Comi,Daniela, AU - Fontana,Gabriele, AU - Martinelli,Marisa, AU - Lorens,James B, AU - Evensen,Lasse, AU - Sironi,Maurizio, AU - Pieraccini,Stefano, AU - Dalla Via,Lisa, AU - Gia,Ornella Maria, AU - Passarella,Daniele, Y1 - 2012/10/19/ PY - 2012/06/28/received PY - 2012/09/13/revised PY - 2012/10/23/entrez PY - 2012/10/23/pubmed PY - 2013/4/30/medline SP - 2134 EP - 43 JF - ChemMedChem JO - ChemMedChem VL - 7 IS - 12 N2 - The introduction of a methylenthiol group at position 7 of camptothecin was carried out in four steps. This preparation also yielded the corresponding disulfide, which behaves as a prodrug due to its reactivity with glutathione. Assessment of their antiproliferative activities, investigations of their mechanism of action, and molecular modeling analysis indicated that the 7-modified camptothecin derivatives described herein maintain the biological activity and drug-target interactions of the parent compound. SN - 1860-7187 UR - https://www.unboundmedicine.com/medline/citation/23086693/Camptothecin_7_yl_methanthiole:_semisynthesis_and_biological_evaluation_ L2 - https://doi.org/10.1002/cmdc.201200322 DB - PRIME DP - Unbound Medicine ER -