Semisynthesis, Biological Activity, and Molecular Modeling Studies of C-Ring-Modified Camptothecins (Articolo in rivista)

Type
Label
  • Semisynthesis, Biological Activity, and Molecular Modeling Studies of C-Ring-Modified Camptothecins (Articolo in rivista) (literal)
Anno
  • 2009-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1021/jm801153y (literal)
Alternative label
  • Varchi, G (1); Samori, C (1); Guerrini, A (1); Fontana, G (3); Bombardelli, E (3); Tinelli, S (2); Beretta, GL (2); Basili, S (4); Moro, S (4); Zunino, F (2); Battaglia, A (1) (2009)
    Semisynthesis, Biological Activity, and Molecular Modeling Studies of C-Ring-Modified Camptothecins
    in Journal of medicinal chemistry (Online)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Varchi, G (1); Samori, C (1); Guerrini, A (1); Fontana, G (3); Bombardelli, E (3); Tinelli, S (2); Beretta, GL (2); Basili, S (4); Moro, S (4); Zunino, F (2); Battaglia, A (1) (literal)
Pagina inizio
  • 1029 (literal)
Pagina fine
  • 1039 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 52 (literal)
Rivista
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • 1. Ist CNR Sintesi Organ & Fotoreattivita ISOF, Area Ric Bologna, I-40129 Bologna, Italy 2. Fdn IRCCS Ist Nazl Tumori, Dipartimento Oncol Sperimentale & Lab, I-20133 Milan, Italy 3. Indena SPA, I-20139 Milan, Italy 4. Univ Padua, Dipartimento Sci Farmaceut, MMS, I-35131 Padua, Italy (literal)
Titolo
  • Semisynthesis, Biological Activity, and Molecular Modeling Studies of C-Ring-Modified Camptothecins (literal)
Abstract
  • The synthesis, biological activity, and molecular modeling studies of C-ring-rnodified camptothecins are reported. A general synthetic protocol, based on \"C-5 camptothecin (C-5-CPT) enolate chemistry\", allows one to obtain various C5-substituted analogues. All new Compounds, obtained as 1:1 epimeric mixtures, were tested for their antiproliferative activity. Experimental data showed that all novel derivatives are less active than the reference compounds and that one of the two epimers; is more active than the other. Molecular docking simulations were performed to achieve more insight into the interactions between the new C5-modified CPTs and Topo I. A good correlation was observed when the data of cytotoxicity and the values calculated for the free binding energy were combined. (literal)
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