Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 10, 2009, Pages 2840-2843

  Giannini, Giuseppe ^a   Marzi, Mauro ^a   Marzo, Maria Di ^a   Battistuzzi, Gianfranco ^a   Pezzi, Riccardo ^a   Brunetti, Tiziana ^a   Cabri, Walter ^a   Vesci, Loredana ^a   Pisano, Claudio ^a  

^a Sigma Tau SpA   (Italy)

Author keywords

Antitumor; Bis indoles; HDAC inhibitors; Hydroxamic acids

Indexed keywords

HISTONE DEACETYLASE INHIBITOR; HYDROXAMIC ACID DERIVATIVE; INDOLE DERIVATIVE; METHANE; VORINOSTAT; ZINC;

ANTINEOPLASTIC ACTIVITY; ARTICLE; DRUG DESIGN; DRUG SYNTHESIS; ENZYME INHIBITION; MOLECULAR RECOGNITION; PHARMACOPHORE;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DRUG DESIGN; ENZYME INHIBITORS; HISTONE DEACETYLASES; HUMANS; HYDROXAMIC ACIDS; INDOLES; PROTEIN STRUCTURE, TERTIARY; SURFACE PROPERTIES;

EID: 65449160954     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.03.101     Document Type: Article

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11. SAHA was in-house synthesized.
12. 50 values of the compounds were determined by analyzing dose-response inhibition curves. Trichostatin A (TSA) was used as reference compound.Screening was performed by Reaction Biology Corp.