Antitumor agents: structure--activity relationships in tenulin series.
Systematic structural modifications were performed on the natural sesquiterpene lactone tenulin to define those groupings essential to, or significant in, its in vivo antitumor activity. Accordingly, the following tenulin analogs were prepared: dihydrotenulin, 2,3-epoxytenulin, isotenulin, dihydroisotenulin, 2,3-epoxyisotenulin, and tetrahydrodeacetylisotenulin. Both the cyclopentenone and the hemiketal units in tenulin were necessary for high in vivo activity.
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000627:therapeutic use; D002279:Carcinoma 256, Walker / Q000188:drug therapy; D005260:Female; D007783:Lactones / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D007942:Leukemia, Experimental / Q000188:drug therapy; D051379:Mice; D051381:Rats; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D007783:Lactones; D012717:Sesquiterpenes; C011124:tenulin