title: Structural requirement of arylindolylpropenones as anti-bladder carcinoma cells agents.
abstract: Chalcones have been identified as interesting compounds with cytotoxicity, anti-inflammatory and antioxidant properties. In the present study, we report the synthesis and evaluation of new 1-(N-methylindolyl)-3-phenylpropenones as anti-cancer agents acting on bladder carcinoma cell line. Among the 15 investigated molecules, three of them inhibit the growth of bladder cancer cells with IC(50) values less than 4 μM after 48 h of treatment. To investigate their mode of action, cell cycle analyses were performed. The most active compounds induce high accumulation at the G2+M phase as assessed by flow cytometry. The structure-activity relationship drawn from the present study highlights the importance of the substitution pattern of the phenyl ring and provides valuable information for further development of this class of compounds as novel anti-cancer chemotherapeutic agents.
authors: AGing Imaging Modeling, FRE 3405, Université Joseph Fourier, CNRS, EPHE, UPMF 38706 La Tronche Cedex, France. Veronique.Frachet@agim.eu
authors: Véronique
authors: V
authors: Martel-Frachet
authors: Malika
authors: M
authors: Kadri
authors: Ahcène
authors: A
authors: Boumendjel
authors: Xavier
authors: X
authors: Ronot
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D047188:Chalcones / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D013329:Structure-Activity Relationship; D001749:Urinary Bladder Neoplasms / Q000188:drug therapy* / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones