THE EFFECT OF 12-ALKOXY MODIFICATION ON THE IN-VITRO ANTILEUKEMIC ACTIVITY OF N-METHYL 2,3,8,9-TETRAMETHOXYBENZO[C]PHENANTHRIDINIUM SALTS

Some members of a series of 12-alkyloxy benzol[c]phenanthridines are p otent inhibitors of the growth of P388 tumour cells in vitro, with a s trong dependence on the nature of the 12-substituent. Analogues with a quaternary nitrogen in the side chain bind strongly to DNA but are le ss active against the tumour cells. The multi-drug-resistant cell line Pr8/22 shows less sensitivity to the new compounds. K562 Human leukae mia cells undergo differentiation in the presence of the benzo[c]phena nthridine derivatives with a structure-activity relationship which doe s not correlate well with potency against the P388 cell line.