1-Amino-substituted 4-methyl-5H-pyrido[3',4':4,5]pyrrolo[3,2-c]pyridines: a new class of antineoplastic agents.
In an attempt to find new anticancer agents, a series of pyrido[3',4':4,5]pyrrolo[3,2-c]pyridines were synthesized and evaluated in the standard NCI screening. Among these new compounds, which are structurally related to 9-azaellipticines but differ by deletion of a cycle, those that have a 4-methyl group and a NHCH2CH2CH2NR2 side chain at the 1-position show significant cytotoxicity on L1210 cultured cells and antitumor properties in the in vivo P388 leukemia system. The in vivo antineoplastic activity of the most potent compounds were confirmed on the L1210 leukemia model.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D002460:Cell Line; D004247:DNA / Q000378:metabolism; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D011725:Pyridines / Q000138:chemical synthesis* / Q000627:therapeutic use; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D011725:Pyridines; D011758:Pyrroles; D004247:DNA