Dimeric analogues of non-cationic tricyclic aromatic carboxamides are a new class of cytotoxic agents.

摘要: A series of tricyclic aromatic carboxamides, and their corresponding dimeric analogues, were prepared growth-inhibitory properties evaluated in a cell lines. The compounds by reaction the appropriate acids with carbonyl-1,1'-diimidazole, isolating resulting imidazolides, reacting these stoichiometric amount diamine. monomeric carboxamides containing (CH 2 ) NMe side chain had widely differing inhibitory potencies, known nitronaphthalimide (mitonafide) acridine-4-carboxamide (DACA) being most potent. bis linked 3 NMe(CH chain, generally more potent, largest increases (dimer/monomer ratio 20- to 30-fold) seen for nitronaphthalimides phenazines. Based on intrinsic cytotoxicity monomers highest degree increase dimerization, interesting chromophores appear be phenazine-1-carboxamide. Both showed significant growth delays (∼6 days) an vivo colon 38 tumour model mice.