[Structure-activity relationship analysis].
All samples for anticancer drug screening were classified according to their structural features and their structure-activity relationships were analyzed. Synthetic gymnastatin analogs including JCI: 11788 and JCI: 11786 altered their selectivity for protein kinase inhibition with the length of a fatty acid chain. Although a new inhibitor of tubulin depolymerization, JCI: 11578, displayed a high correlation to known tubulin binders, novel inhibitors of tubulin polymerization, JCI: 11534, JCI: 11675 and JCI: 11676, exhibited poor correlations to tubulin binders. JCI: 11403 and JCI: 11407 inhibited topoisomerase I selectively and appear to belong to a new family of topoisomerase inhibitors. They are expected to be important key compounds for structure-activity relationship analysis as well as new lead compounds for anticancer drugs.
Hayakawa
Yoichi
Y
Institute of Molecular and Cellular Biosciences, University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
D000970:Antineoplastic Agents / Q000737:chemistry*; D001549:Benzamides; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000737:chemistry; D000077143:Docetaxel; D004354:Drug Screening Assays, Antitumor; D034261:Epothilones / Q000737:chemistry; D000077156:Gefitinib; D000068877:Imatinib Mesylate; D000077146:Irinotecan; D018942:Macrolides; D009842:Oligopeptides / Q000737:chemistry; D017239:Paclitaxel / Q000737:chemistry; D010879:Piperazines / Q000737:chemistry*; D011743:Pyrimidines / Q000737:chemistry*; D011799:Quinazolines / Q000737:chemistry*; D013329:Structure-Activity Relationship; D043823:Taxoids / Q000737:chemistry; D019772:Topotecan / Q000737:chemistry; D014747:Vinblastine / Q000737:chemistry
D000970:Antineoplastic Agents; D001549:Benzamides; D034261:Epothilones; D018942:Macrolides; D009842:Oligopeptides; D010879:Piperazines; D011743:Pyrimidines; D011799:Quinazolines; D043823:Taxoids; C117305:laulimalide; D000077143:Docetaxel; D014747:Vinblastine; D000077146:Irinotecan; D019772:Topotecan; D000068877:Imatinib Mesylate; C105791:soblidotin; D017239:Paclitaxel; D000077156:Gefitinib; C093788:epothilone B; D002166:Camptothecin