Ra. Aitken et al., SYNTHESIS AND ANTITUMOR-ACTIVITY OF NEW DERIVATIVES OF FLAVONE-8-ACETIC ACID (FAA) .2. RING-SUBSTITUTED DERIVATIVES, Archiv der pharmazie, 330(7), 1997, pp. 215-224
A range of 18 derivatives of flavone-8-acetic acid (FAA) with substitu
ents on the 2-phenyl group have been prepared and their anti-tumour ac
tivity evaluated in vitro against a panel of human and murine tumour c
ell lines and in vivo against MAC 15A. There was no clear-cut relation
ship between in vitro and in vivo activity but the activity in each si
tuation was found to be very sensitive to the precise substitution pat
tern with closely related isomers giving widely different activities.
Some of the compounds, notably 10b,c,j, and r, were active in vivo and
these require further studies in order to evaluate their potential fo
r development.