Anticancer activities of novel chalcone and bis-chalcone derivatives.
A series of novel chalcones and bis-chalcones containing boronic acid moieties has been synthesized and evaluated for antitumor activity against the human breast cancer MDA-MB-231 (estrogen receptor-negative) and MCF7 (estrogen receptor-positive) cell lines and against two normal breast epithelial cell lines, MCF-10A and MCF-12A. These molecules inhibited the growth of the human breast cancer cell lines at low micromolar to nanomolar concentrations, with five of them (1-4, 9) showing preferential inhibition of the human breast cancer cell lines. Furthermore, bis-chalcone 8 exhibited a more potent inhibition of colon cancer cells expressing wild-type p53 than of an isogenic cell line that was p53-null.
Modzelewska
Aneta
A
Division of Chemical Therapeutics, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, MD 21231, USA.
Pettit
Catherine
C
Achanta
Geetha
G
Davidson
Nancy E
NE
Huang
Peng
P
Khan
Saeed R
SR
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001897:Boronic Acids / Q000737:chemistry* / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D050150:Chalones / Q000737:chemistry* / Q000494:pharmacology*; D003110:Colonic Neoplasms / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D007928:Lethal Dose 50; D015394:Molecular Structure; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology*
C512278:3,5-bis(4-boronic acid-benzylidene)-1-methylpiperidin-4-one; D000970:Antineoplastic Agents; D001897:Boronic Acids; D050150:Chalones; D010880:Piperidines