Synthesis and biological characterization of amidopropenyl hydroxamates as HDAC inhibitors

ChemMedChem

Volumn 5, Issue 8, 2010, Pages 1359-1372

  Thaler, Florian ^a,e   Varasi, Mario ^b,e   Colombo, Andrea ^c   Boggio, Roberto ^a   Munari, Davide ^b   Regalia, Nickolas ^c   Rozio, Marco G ^c   Reali, Veronica ^c   Resconi, Anna E ^c   Mai, Antonello ^d   Gagliardi, Stefania ^c   Dondio, Giulio ^c   Minucci, Saverio ^e,f   Mercurio, Ciro ^b  

^a Genextra Group   (Italy)

^b Genextra Group   (Italy)

^c NiKem Research   (Italy)

^d SAPIENZA UNIVERSITY OF ROME   (Italy)

^e EUROPEAN INSTITUTE OF ONCOLOGY   (Italy)

^f UNIVERSITY OF MILAN   (Italy)

Author keywords

Antiproliferation; Histone deacetylases; Hydroxamates; Metabolism; Pharmacokinetics

Indexed keywords

AMIDOPROPENYL HYDROXAMATE DERIVATIVE; HISTONE DEACETYLASE 1; HISTONE DEACETYLASE 2; HISTONE DEACETYLASE INHIBITOR; KETONE DERIVATIVE; N HYDROXY 3 (6 ((E) 3 (3 (3 FLUOROPHENYL) PIPERIDIN 1 YL] 3 OXO 1 PROPEN 1 YL] PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [3 ((E) 3 (4 METHYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN 1 YL) PHENYL] ACRYLAMIDE; N HYDROXY 3 [3 ((E) 3 (4 PHENYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN 1 YL) PHENYL] ACRYLAMIDE; N HYDROXY 3 [4 ((E) 3 (4 METHYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN 1 YL) PHENYL] ACRYLAMIDE; N HYDROXY 3 [4 ((E) 3 (4 PHENYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN 1 YL) PHENYL] ACRYLAMIDE; N HYDROXY 3 [4 [(E) 3 (4 METHYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 ((S) 3 PHENYLPIPERIDIN 1 YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (3 (2 METHOXYPHENYL) PIPERIDIN 1 YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (3 (2 TOLYL) PIPERIDIN 1 YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (3 (3 METHOXYPHENYL) PIPERIDIN-1-YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (3 (4 TOLYL) PIPERIDIN 1 YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (3 NAPHTHALEN 1 YL PIPERIDIN 1 YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (3 NAPHTHALEN 2 YLPIPERIDIN 1 YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (3 PHENYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN 1 YL] PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (3 PHENYLPIPERIDIN 1 YL) 3 OXO 1 PROPEN 1 YL] PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (4 METHYL 3 PHENYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN YL] PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (4 METHYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (4 PHENYLAZEPAN 1 YL) 3 OXO 1 PROPEN 1 YL] PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (4 PHENYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN 1 YL) PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 (4 PHENYLPIPERAZIN 1 YL) 3 OXO 1 PROPEN 1 YL] PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 [3 (2 FLUOROPHENYL) PIPERIDIN 1 YL] 3 OXO 1 PROPEN 1 YL] PYRIDIN 2 YL] ACRYLAMIDE; N HYDROXY 3 [6 ((E) 3 [3 (4 METHOXYPHENYL) PIPERIDIN 1 YL] 3 OXO 1 PROPEN 1YL) PYRIDIN 2 YL] ACRYLAMIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; AREA UNDER THE CURVE; ARTICLE; DRUG ACTIVITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG SELECTIVITY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; LIVER CELL; MICROSOME; NONHUMAN; PRIORITY JOURNAL; RAT; TUMOR CELL;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DRUG SCREENING ASSAYS, ANTITUMOR; HISTONE DEACETYLASE INHIBITORS; HISTONE DEACETYLASES; HUMANS; HYDROXAMIC ACIDS; MICE; MICROSOMES, LIVER; PROTEIN ISOFORMS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77955098441     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201000166     Document Type: Article

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