Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
Compounds 1-5, structurally related to combretastatin A-4 showed excellent cytotoxic activities against a panel of human cancer cell lines including multi-drug resistant cell lines. The X-ray three-dimensional structural analysis shows that proton donor in B ring may be required for cytotoxic activity, with intermolecular hydrogen bonding playing an important role.
Hsieh
Hsing-Pang
HP
Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 9F, 161, Sec. 6, Min-Chiuan East Road, Taipei 114, Taiwan, ROC. hphsieh@nhri.org.tw
Liou
Jing-Ping
JP
Lin
Ying-Ting
YT
Mahindroo
Neeraj
N
Chang
Jang-Yang
JY
Yang
Yung-Ning
YN
Chern
Shuenn-Shing
SS
Tan
Uan-Kang
UK
Chang
Chun-Wei
CW
Chen
Tung-Wei
TW
Lin
Chi-Hung
CH
Chang
Ying-Ying
YY
Wang
Chiung-Chiu
CC
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D001577:Benzophenones / Q000138:chemical synthesis* / Q000494:pharmacology; D001632:Bibenzyls / Q000737:chemistry; D002453:Cell Cycle / Q000187:drug effects; D018360:Crystallography, X-Ray; D018432:Drug Resistance, Multiple; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D013267:Stilbenes; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D001577:Benzophenones; D001632:Bibenzyls; D013267:Stilbenes; C040105:combretastatin