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Synthesis and cytotoxic activity of new 9-substituted camptothecins.
Bioorg Med Chem Lett. 2008 May 01; 18(9):2781-7.BM

Abstract

A series of novel 9-substituted camptothecins derived from 9-formylcamptothecin were synthesized. The aldehyde was obtained from 10-hydroxycamptothecin or, better, by total synthesis. The compounds showed antiproliferative activity higher than that of the reference compound topotecan. Modelling suggested the possibility of a favourable interaction of small and polar 9-substituents with the topoisomerase I-DNA complex, which is consistent with the higher activity of these derivatives with respect to the corresponding 7-substituted camptothecins.

Authors+Show Affiliations

Dipartimento di Scienze Molecolari Agroalimentari, Università di Milano, Via Celoria 2, 20133 Milano, Italy. sabrina.dallavalle@unimi.itNo 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

18434153

Citation

Dallavalle, Sabrina, et al. "Synthesis and Cytotoxic Activity of New 9-substituted Camptothecins." Bioorganic & Medicinal Chemistry Letters, vol. 18, no. 9, 2008, pp. 2781-7.
Dallavalle S, Rocchetta DG, Musso L, et al. Synthesis and cytotoxic activity of new 9-substituted camptothecins. Bioorg Med Chem Lett. 2008;18(9):2781-7.
Dallavalle, S., Rocchetta, D. G., Musso, L., Merlini, L., Morini, G., Penco, S., Tinelli, S., Beretta, G. L., & Zunino, F. (2008). Synthesis and cytotoxic activity of new 9-substituted camptothecins. Bioorganic & Medicinal Chemistry Letters, 18(9), 2781-7. https://doi.org/10.1016/j.bmcl.2008.04.016
Dallavalle S, et al. Synthesis and Cytotoxic Activity of New 9-substituted Camptothecins. Bioorg Med Chem Lett. 2008 May 1;18(9):2781-7. PubMed PMID: 18434153.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and cytotoxic activity of new 9-substituted camptothecins. AU - Dallavalle,Sabrina, AU - Rocchetta,Daniela Granza, AU - Musso,Loana, AU - Merlini,Lucio, AU - Morini,Gabriella, AU - Penco,Sergio, AU - Tinelli,Stella, AU - Beretta,Giovanni Luca, AU - Zunino,Franco, Y1 - 2008/04/10/ PY - 2008/03/14/received PY - 2008/04/04/revised PY - 2008/04/06/accepted PY - 2008/4/25/pubmed PY - 2008/7/17/medline PY - 2008/4/25/entrez SP - 2781 EP - 7 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 18 IS - 9 N2 - A series of novel 9-substituted camptothecins derived from 9-formylcamptothecin were synthesized. The aldehyde was obtained from 10-hydroxycamptothecin or, better, by total synthesis. The compounds showed antiproliferative activity higher than that of the reference compound topotecan. Modelling suggested the possibility of a favourable interaction of small and polar 9-substituents with the topoisomerase I-DNA complex, which is consistent with the higher activity of these derivatives with respect to the corresponding 7-substituted camptothecins. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/18434153/Synthesis_and_cytotoxic_activity_of_new_9_substituted_camptothecins_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(08)00407-1 DB - PRIME DP - Unbound Medicine ER -