http://www.cnr.it/ontology/cnr/individuo/prodotto/ID181811
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)
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- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
- 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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