One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5- (3′,4′,5′-trimethoxybenzoyl)thiazole: A unique, highly active antimicrotubule agent

European Journal of Medicinal Chemistry

Volumn 46, Issue 12, 2011, Pages 6015-6024

  Romagnoli, Romeo ^a   Baraldi, Pier Giovanni ^a   Lopez Cara, Carlota ^a   Kimatrai Salvador, Maria ^a   Bortolozzi, Roberta ^b   Basso, Giuseppe ^b   Viola, Giampietro ^b   Balzarini, Jan ^c   Brancale, Andrea ^d   Fu, Xian Hua ^e   Li, Jun ^e   Zhang, Su Zhan ^e   Hamel, Ernest ^f  

^a UNIVERSITY OF FERRARA   (Italy)

^b UNIVERSITY OF PADOVA   (Italy)

^c REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

^d CARDIFF UNIVERSITY   (United Kingdom)

^e ZHEJIANG UNIVERSITY   (China)

^f NATIONAL CANCER INSTITUTE   (United States)

Author keywords

In vivo and in vitro activity; Microtubules; Structure activity relationship; Thiazole; Tubulin

Indexed keywords

(4 AMINO 2 PYRROLIDIN 1 YL 1,3 THIAZOL 5 YL)(3,4,5 TRIMETHOXYPHENYL)METHANONE; ANTIMITOTIC AGENT; CASPASE 3; COLCHICINE; COMBRETASTATIN A4; DOXORUBICIN; PACLITAXEL; PROTEIN BAX; PROTEIN BCL 2; THIAZOLE DERIVATIVE; TUBULIN; UNCLASSIFIED DRUG; VINBLASTINE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; CANCER INHIBITION; CELL CYCLE G2 PHASE; CELL CYCLE M PHASE; CELL INTERACTION; CELL MEMBRANE DEPOLARIZATION; CELL PROLIFERATION; CELL STRAIN HT29; CONCENTRATION RESPONSE; CONTROLLED STUDY; CYTOTOXICITY; DRUG SCREENING; ENZYME ACTIVATION; FEMALE; HELA CELL; HUMAN; HUMAN CELL; HYDROPHOBICITY; IC 50; IN VITRO STUDY; IN VIVO STUDY; MICROTUBULE ASSEMBLY; MITOSIS INHIBITION; MOLECULAR MODEL; MOUSE; MULTIDRUG RESISTANCE; NONHUMAN; ONE POT SYNTHESIS; PARTICLE SIZE; PROTEIN BINDING; PROTEIN EXPRESSION; TUMOR VOLUME; XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; CASPASE 3; CELL LINE, TUMOR; CELL PROLIFERATION; FEMALE; G2 PHASE; HELA CELLS; HUMANS; MICE; MICE, INBRED BALB C; MICE, NUDE; NEOPLASMS; THIAZOLES; TUBULIN; TUBULIN MODULATORS;

EID: 80955166264     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2011.10.013     Document Type: Article

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