Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors

Journal of Medicinal Chemistry

Volumn 53, Issue 2, 2010, Pages 822-839

  Thaler, Florian ^a,d   Colombo, Andrea ^b   Mai, Antonello ^c   Amici, Raffaella ^a,d   Bigogno, Chiara ^b   Boggio, Roberto ^a   Cappa, Anna ^a,d   Carrara, Simone ^b   Cataudella, Tiziana ^a   Fusar, Fulvia ^a   Gianti, Eleonora ^a,d   Di Ventimiglia, Samuele Joppolo ^b   Moroni, Maurizio ^a   Munari, Davide ^a   Pain, Gilles ^a,f   Regalia, Nickolas ^b   Sartori, Luca ^a,d   Vultaggio, Stefania ^a   Dondio, Giulio ^b   Gagliardi, Stefania ^b   Minucci, Saverio ^d,e   Mercurio, Ciro ^a   Varasi, Mario ^a,d   more..

^a Genextra Group   (Italy)

^b NiKem srl   (Italy)

^c SAPIENZA UNIVERSITY OF ROME   (Italy)

^d EUROPEAN INSTITUTE OF ONCOLOGY   (Italy)

^e UNIVERSITY OF MILAN   (Italy)

^f Sigma Tau SpA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

CASPASE 3; CASPASE 7; HISTONE DEACETYLASE INHIBITOR; N HYDROXY 3 [5 [3 [2 (4 METHYLPIPERAZIN 1 YL)PHENYL] 3 OXO 1 PROPEN 1 YL]PYRIDIN 2 YL]ACRYLAMIDE; N HYDROXYPHENYLACRYLAMIDE DERIVATIVE; N HYDROXYPYRIDIN 2 YLACRYLAMIDE DERIVATIVE; UNCLASSIFIED DRUG; VORINOSTAT;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CANCER CELL CULTURE; CANCER INHIBITION; CELL STRAIN HCT116; CELL STRAIN K 562; CONTROLLED STUDY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG STABILITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IC 50; MALE; MOUSE; NONHUMAN; NUDE MOUSE; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION;

ACRYLAMIDES; ANTINEOPLASTIC AGENTS; BENZENE DERIVATIVES; CELL PROLIFERATION; COLONIC NEOPLASMS; DRUG STABILITY; ENZYME INHIBITORS; HELA CELLS; HISTONE DEACETYLASE INHIBITORS; HUMANS; PYRIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 77249133651     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm901502p     Document Type: Article

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