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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.

Authors+Show Affiliations

Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy.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 availableNo affiliation info available

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 -