Synthesis and anticancer evaluation of thiazolyl-chalcones.
Thirty-seven (E)-1-(4-methyl-2-arylaminothiazol-5-yl)-3-arylprop-2-en-1-ones were synthesized via Claisen-Schmidt condensation of 1-(4-methyl-2-(arylamino)thiazol-5-yl)ethanone with the corresponding arylaldehydes. All these thiazolyl-chalcones were characterized and evaluated by MTT assay on human cancer cell lines BGC-823, PC-3, NCI-H460, BEL-7402 in vitro. Compounds 5, 8, 26, 37 and 41 are effective against cancer cell lines with IC(50)s below 10 μM. The antitumor activity in ICR mice bearing sarcoma 180 tumors indicates compounds 10 and 41 have moderate in vivo activity with 22-25% tumor-weight inhibition.
Shi
Hai-Bo
HB
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310032, PR China.
Zhang
Shi-Jie
SJ
Ge
Qiu-Fu
QF
Guo
Dian-Wu
DW
Cai
Chao-Ming
CM
Hu
Wei-Xiao
WX
D000818:Animals; D045744:Cell Line, Tumor; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008813:Mice, Inbred ICR; D013844:Thiazoles / Q000737:chemistry*
D047188:Chalcones; D013844:Thiazoles