Synthesis and antitumor activity of pyrido-amsacrine analogues and related compounds.
The pyrido derivatives of amsacrine [4'-(9-acridinylamino) methanesulfon-m-anisidine] were prepared and evaluated in the L1210 leukemia system. Almost all the pyrido analogues were tighter DNA-binding ligands than the corresponding amsacrine compounds. The significant inhibition of L1210 produced by pyrido-acridan-7-ones demonstrates that the anilino side chain is not essential for activity, although most of the compounds did not have improved activity compared with amsacrine.
Llama
E
E
Departmento de Quimica Organica y Farmaceutica, Facultad de Farmacia, Universidad Complutense, Madrid, Spain.
Del Campo
C
C
Capo
M
M
Anadon
M
M
D000677:Amsacrine / Q000031:analogs & derivatives*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D004273:DNA, Neoplasm / Q000187:drug effects / Q000378:metabolism; D004355:Drug Stability; D007939:Leukemia L1210 / Q000188:drug therapy / Q000378:metabolism; D051379:Mice; D009368:Neoplasm Transplantation; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004273:DNA, Neoplasm; D000677:Amsacrine