Synthesis and anti-cancer activity of chalcone linked imidazolones.
A series of novel chalcone linked imidazolones were prepared and evaluated for their anti-cancer activity against a panel of 53 human tumour cell lines derived from nine different cancer types: leukemia, lung, colon, CNS, melanoma, ovarian, renal, prostate and breast. Some of these hybrids (6, 7 and 8) showed good anti-cancer activity with GI(50) values ranging from 1.26 to 13.9 microM. When breast carcinoma cells (MCF-7) were treated with 10 microM concentration of compounds TMAC, CA-4, 6 and 8 cell cycle arrest was observed in G2/M phase. Surprisingly, the increased concentration of the same compound to 30 microM caused accumulation of cells in G0/G1 phase of the cell cycle.
Kamal
Ahmed
A
Chemical Biology Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India. ahmedkamal@iict.res.in
Ramakrishna
G
G
Raju
P
P
Viswanath
A
A
Ramaiah
M Janaki
MJ
Balakishan
G
G
Pal-Bhadra
Manika
M
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D045744:Cell Line, Tumor; D002599:Chalcone / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D009369:Neoplasms / Q000188:drug therapy*
D000970:Antineoplastic Agents; D007093:Imidazoles; C117197:imidazolone; D002599:Chalcone