New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies. (Articolo in rivista)

Type

• Articolo in rivista (Classe)
• Prodotto della ricerca (Classe)

Label

• New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies. (Articolo in rivista) (literal)

Anno

• 2009-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

• 10.1021/jm900016t (literal)

Alternative label

• La Regina G; Sarkar T; Bai R; Edler MC; Saletti R; Coluccia A; Piscitelli F; Minelli L; Gatti V; Mazzoccoli C; Palermo V; Mazzoni C; Falcone C; Scovassi AI; Giansanti V; Campiglia P; Porta A; Maresca B; Hamel E; Brancale A; Novellino E; Silvestri R. (2009)
  New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies.
  in Journal of medicinal chemistry
  (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

• La Regina G; Sarkar T; Bai R; Edler MC; Saletti R; Coluccia A; Piscitelli F; Minelli L; Gatti V; Mazzoccoli C; Palermo V; Mazzoni C; Falcone C; Scovassi AI; Giansanti V; Campiglia P; Porta A; Maresca B; Hamel E; Brancale A; Novellino E; Silvestri R. (literal)

Pagina inizio

• 7512 (literal)

Pagina fine

• 7527 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#url

• http://pubs.acs.org/doi/abs/10.1021/jm900016t (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

• 52 (literal)

Rivista

• Journal of medicinal chemistry (Rivista)

Note

• PubMe (literal)
• Scopus (literal)
• ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

• La Regina G; Coluccia A; Piscitelli F; Minelli L; Gatti V; Mazzoccoli C; Palermo V, Mazzoni C, Falcone C, Campiglia P, Silvestri R: La Sapienza Università, Roma Novellino E: Università di Napoli Porta A, Maresca B: Università di Salerno Saletti R; Brancale A: Cardiff University, UK Sarkar T; Bai R; Edler MC; Hamel E: NIH, USA Scovassi AI, Giansanti V: IGM-CNR (literal)

Titolo

• New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies. (literal)

Abstract

• New arylthioindoles along with the corresponding ketone and methylene compounds were potent tubulin assembly inhibitors. As growth inhibitors of MCF-7 cells, sulfur derivatives were superior or sometimes equivalent to the ketones, while methylene derivatives were substantially less effective. Esters 24, 27-29, 36, 39, and 41 showed approximately 50% of inhibition on human HeLa and HCT116/chr3 cells at 0.5 muM, and these compounds inhibited the growth of HEK, M14, and U937 cells with IC(50)'s in the 78-220 nM range. While murine macrophage J744.1 cell growth was significantly less affected (20% at higher concentrations), four other nontransformed cell lines remained sensitive to these esters. The effect of drug treatment on cell morphology was examined by time-lapse microscopy. In a protocol set up to evaluate toxicity on the Saccharomyces cerevisiae BY4741 wild type strain, compounds 24 and 54 strongly reduced cell growth, and 29, 36, and 39 also showed significant inhibition. (literal)

Prodotto di

• Institute of molecular genetics (IGM) (Istituto)
• Cromosomi artificiali per terapia genica. Studi sulla replicazione del DNA in cellule umane ; controllo del ciclo cellulare e della proliferazione. (ME.P05.006.001) (Modulo)

Autore CNR

• ANNA SCOVASSI (Unità di personale interno)

Insieme di parole chiave

• Keywords of "New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies." (Insieme di parole chiave)

Incoming links:

Prodotto

• Institute of molecular genetics (IGM) (Istituto)
• Cromosomi artificiali per terapia genica. Studi sulla replicazione del DNA in cellule umane ; controllo del ciclo cellulare e della proliferazione. (ME.P05.006.001) (Modulo)

Autore CNR di

• ANNA SCOVASSI (Unità di personale interno)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi

• Journal of medicinal chemistry (Rivista)

Insieme di parole chiave di

• Keywords of "New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies." (Insieme di parole chiave)