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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.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Dallavalle S
Dipartimento di Scienze Molecolari Agroalimentari, Università di Milano, Via Celoria 2, 20133 Milano, Italy. sabrina.dallavalle@unimi.it
Rocchetta DG
No affiliation info available
Musso L
No affiliation info available
Merlini L
No affiliation info available
Morini G
No affiliation info available
Penco S
No affiliation info available
Tinelli S
No affiliation info available
Beretta GL
No affiliation info available
Zunino F
No affiliation info available

MeSH

Antineoplastic Agents, PhytogenicCamptothecinCell SurvivalDNA Topoisomerases, Type IDrug Screening Assays, AntitumorHumansStructure-Activity RelationshipTumor Cells, Cultured

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_ DB - PRIME DP - Unbound Medicine ER -