Antitumor and immunosuppressive activities of lankacidin-group antibiotics: structure-activity relationships.
The antitumor and immunosuppressive activities of the lankacidin-group antibiotics were studied in mice. Seventeen of 29 newly prepared lankacidin-group antibiotics, including 14-derivatives of lankacidin C, lankacidinol, isolankacidinol, and lankacidinol 14-acetate, possessed considerable antitumor activity against ascites 6C3HED/OG lymphosarcoma. Comparative studies on the antitumor activity of lankacidin C and eight of its derivatives against L1210 leukemia and solid 6C3HED/OG lymphosarcoma demonstrated that replacement of the hydroxyl group at position 8 or 14 of lankacidin C by an acyloxy group potentiated antitumor activity. However, these modifications of lankacidin C resulted in reduction of the immunosuppressive activity.
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology / Q000627:therapeutic use; D000917:Antibody Formation / Q000187:drug effects; D004912:Erythrocytes / Q000276:immunology; D005260:Female; D006087:Graft vs Host Reaction / Q000187:drug effects; D007166:Immunosuppressive Agents; D007783:Lactones / Q000494:pharmacology / Q000627:therapeutic use; D007939:Leukemia L1210 / Q000188:drug therapy; D008228:Lymphoma, Non-Hodgkin / Q000188:drug therapy; D008297:Male; D051379:Mice; D008809:Mice, Inbred C3H; D008810:Mice, Inbred C57BL; D008811:Mice, Inbred DBA; D012513:Sarcoma, Experimental / Q000188:drug therapy; D012756:Sheep / Q000276:immunology; D013154:Spleen / Q000637:transplantation; D013329:Structure-Activity Relationship
D000903:Antibiotics, Antineoplastic; D007166:Immunosuppressive Agents; D007783:Lactones