title: 2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
abstract: The essential role of microtubules in mitosis makes them a major target of compounds useful for cancer therapy. In our search for potent antitumor agents, a novel series of 2-anilino-4-amino-5-aroylthiazoles was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. SAR was elucidated with various substitutions on the phenylamino and aroyl moiety at the 2- and 5-positions, respectively, of the 4-aminothiazole skeleton. Tumor cell exposure to several of these compounds led to the arrest of HeLa cells in the G2/M phase of the cell cycle and induction of apoptosis.
authors: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Ferrara, Italy. rmr@unife.it
authors: Romeo
authors: R
authors: Romagnoli
authors: Pier Giovanni
authors: PG
authors: Baraldi
authors: Maria Dora
authors: MD
authors: Carrion
authors: Olga
authors: O
authors: Cruz-Lopez
authors: Carlota Lopez
authors: CL
authors: Cara
authors: Giuseppe
authors: G
authors: Basso
authors: Giampietro
authors: G
authors: Viola
authors: Mohammed
authors: M
authors: Khedr
authors: Jan
authors: J
authors: Balzarini
authors: Siavosh
authors: S
authors: Mahboobi
authors: Andreas
authors: A
authors: Sellmer
authors: Andrea
authors: A
authors: Brancale
authors: Ernest
authors: E
authors: Hamel
mesh_terms: D002460:Cell Line; D004583:Electrons; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D055503:Protein Multimerization / Q000187:drug effects*; D020836:Protein Structure, Quaternary; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014404:Tubulin / Q000737:chemistry / Q000378:metabolism*
chemical_list: D013844:Thiazoles; D014404:Tubulin