Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability

Journal of Medicinal Chemistry

Volumn 54, Issue 24, 2011, Pages 8394-8406

  La Regina, Giuseppe ^a   Bai, Ruoli ^b   Rensen, Willeke ^a   Coluccia, Antonio ^a   Piscitelli, Francesco ^a   Gatti, Valerio ^a   Bolognesi, Alessio ^a   Lavecchia, Antonio ^e   Granata, Ilaria ^c   Porta, Amalia ^c   Maresca, Bruno ^c   Soriani, Alessandra ^a   Iannitto, Maria Luisa ^a   Mariani, Marisa ^f   Santoni, Angela ^a   Brancale, Andrea ^d   Ferlini, Cristiano ^f   Dondio, Giulio ^g   Varasi, Mario ^h   Mercurio, Ciro ⁱ   Hamel, Ernest ^b   Lavia, Patrizia ^a   Novellino, Ettore ^e   Silvestri, Romano ^a   more..

^a SAPIENZA UNIVERSITY OF ROME   (Italy)

^b NATIONAL INSTITUTES OF HEALTH   (United States)

^c UNIVERSITY OF SALERNO   (Italy)

^d CARDIFF UNIVERSITY   (United Kingdom)

^e UNIVERSITY OF NAPLES FEDERICO II   (Italy)

^f DANBURY HOSPITAL   (United States)

^g NiKem Research   (Italy)

^h EUROPEAN INSTITUTE OF ONCOLOGY   (Italy)

ⁱ DAC SRL   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2 (1H PYRROL 2 YL) 3 [(3',4',5' TRIMETHOXYPHENYL)THIO] 1H INDOLE; 2 (1H PYRROL 3 YL) 3 [(3',4',5' TRIMETHOXYPHENYL)THIO] 1H INDOLE; 2 (FURAN 2 YL) 3 [(3',4',5' TRIMETHOXYPHENYL)THIO] 1H INDOLE; 2 (FURAN 3 YL) 3 [(3',4',5' TRIMETHOXYPHENYL)THIO] 1H INDOLE; 2 (THIOPHEN 2 YL) 3 (3',4',5' TRIMETHOXYBENZYL) 1H INDOLE; 2 (THIOPHEN 2 YL) 3 [(3',4',5' TRIMETHOXYPHENYL)THIO] 1H INDOLE; 2 (THIOPHEN 3 YL) 3 [(3',4',5' TRIMETHOXYPHENYL)THIO] 1H INDOLE; 5 METHOXY 2 (THIOPHEN 2 YL) 3 [(3',4',5' TRIMETHOXYPHENYL)THIO] 1H INDOLE; [2 (THIOPHEN 2 YL) 1H INDOL 3 YL](3',4',5' TRIMETHOXYPHENYL)METHANONE; ANTINEOPLASTIC AGENT; CASPASE 3; CISPLATIN; COLCHICINE; COMBRETASTATIN A4; DOXORUBICIN; ETHOXYCOUMARIN; GLYCOPROTEIN P; INDOLE DERIVATIVE; NAVELBINE; PACLITAXEL; PROPRANOLOL; PROTEIN P53; TUBULIN; UNCLASSIFIED DRUG; VINBLASTINE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; AREA UNDER THE CURVE; ARTICLE; CANCER CELL CULTURE; CELL CYCLE ARREST; CELL VIABILITY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG METABOLISM; DRUG SOLUBILITY; DRUG STABILITY; DRUG SYNTHESIS; EMBRYO; ENZYME INDUCTION; FEMALE; GENE OVEREXPRESSION; HUMAN; HUMAN CELL; IC 50; LIVER METABOLISM; LIVER MICROSOME; MALE; MAXIMUM PLASMA CONCENTRATION; MICROWAVE RADIATION; MITOSIS; MOUSE; NONHUMAN; PROTEIN EXPRESSION; PROTEIN POLYMERIZATION; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BIOLOGICAL AVAILABILITY; CASPASE 3; CELL CYCLE; CELL LINE; CELL LINE, TUMOR; CELL PROLIFERATION; DRUG DESIGN; DRUG RESISTANCE, NEOPLASM; DRUG SCREENING ASSAYS, ANTITUMOR; FURANS; HUMANS; INDOLES; INJECTIONS, INTRAVENOUS; MALE; MICE; MICE, NUDE; MICROSOMES, LIVER; PYRROLES; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES; TUBULIN MODULATORS;

EID: 84055211830     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2012886     Document Type: Article

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