The effect of 12-alkoxy modification on the in vitro antileukaemic activity of N-methyl 2,3,8,9-tetramethoxybenzo[c]phenanthridinium salts.
Some members of a series of 12-alkyloxy benzo[c]phenanthridines are potent inhibitors of the growth of P388 tumour cells in vitro, with a strong dependence on the nature of the 12-substituent. Analogues with a quaternary nitrogen in the side chain bind strongly to DNA but are less active against the tumour cells. The multi-drug-resistant cell line Pr8/22 shows less sensitivity to the new compounds. K562 Human leukaemia cells undergo differentiation in the presence of the benzo[c]phenanthridine derivatives with a structure-activity relationship which does not correlate well with potency against the P388 cell line.
Mackay
S P
SP
School of Health Sciences, University of Sunderland, UK.
Comoe
L
L
Desoize
B
B
Duval
O
O
Jardillier
J C
JC
Waigh
R D
RD
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D020014:K562 Cells / Q000187:drug effects; D007938:Leukemia / Q000188:drug therapy*; D007941:Leukemia P388 / Q000188:drug therapy; D010617:Phenanthridines / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D010617:Phenanthridines