Synthesis and anti-tumor activity of novel combretastatins: combretocyclopentenones and related analogues.
A series of 2-(3,4,5-trimethoxyphenyl)-3-arylcyclopent-2-ene-1-ones (8a-8e) and their related analogues, including pentenone 9a, pentenol 10a, pentene 12a, and furane 15, were synthesized and evaluated for cytotoxicity against murine and human tumor cell lines. Compounds 8a-c, 8e and 9a showed strong cytotoxicity with IC(50) values in the range of 8-34ng/mL. Compound 8e exhibited significant anti-tumor activity in BDF1 mice bearing Lewis lung carcinoma cells with an inhibition ratio of 59%.
College of Pharmacy, Chungnam National University, Taejon 305-764, Republic of Korea.
Nguyen-Hai
NH
Nam
Yong
Y
Kim
Young-Jae
YJ
You
Dong-Ho
DH
Hong
Hwan-Mook
HM
Kim
Byung-Zun
BZ
Ahn
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001632:Bibenzyls / Q000138:chemical synthesis* / Q000494:pharmacology*; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy; D003517:Cyclopentanes / Q000737:chemistry* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D013237:Stereoisomerism; D013267:Stilbenes; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D001632:Bibenzyls; D003517:Cyclopentanes; D013267:Stilbenes; C040105:combretastatin; C013905:cyclopentenone