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.
Links
MeSH
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 -