The synthesis, and growth inhibition studies against the L1210 mouse l
eukaemia, MCF-7 human breast cancer and SKOV-3 ovarian carcinoma cell
lines, of derivatives of lithocholic acid and cholic acid in which qui
noline-3-carboxylate and acridine-9-carboxylate are substituted at the
3 and/or the 24 position are reported. The 3 alpha,24-diheteroaryl-su
bstituted steroid systems, lithocholic acid, cholic acid, quinoline an
d acridine-9-carboxylic acid showed no significant biological activity
against any of the cell lines. In contrast, when either a single quin
oline-3-carboxylate or acridine-9-carboxylate unit is substituted onto
position 24 of the steroid derivatives, significant activity against
L1210, and weak activity against the MCF-7 and SKOV-3 lines is exhibit
ed. DNA thermal denaturation studies of these compounds showed no dete
ctable binding to calf thymus DNA.