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Anticancer Potential of 3-(Arylideneamino)-2- Phenylquinazoline-4(3H)-One Derivatives
Different quinazoline derivatives have showed wide
spectrum of pharmacological activities. Some 3-
(arylideneamino)-phenylquinazoline-4(3H)-ones have
been reported to possess antimicrobial activity. The
present study has been undertaken to evaluate the
anticancer effect of these quinazolinone derivatives.
The quinazolinone derivatives were synthesized as
reported earlier. Compounds containing NO2, OH,
OCH3, or OH and OCH3 as substituent(s) on the
arylideneamino group were named as P(3a), P(3b),
P(3c), and P(3d) respectively. Out of these, P(3a)
and P(3d) showed better cytotoxic activity than P(3b)
and P(3c) on a panel of six cancer cell lines of different
origin, namely, B16F10, MiaPaCa-2, HCT116, HeLa,
MCF7, and HepG2, though the effect was higher in
B16F10, HCT116, and MCF7 cells. P(3a) and P(3d)
induced death of B16F10 and HCT116 cells was
associated with characteristic apoptotic changes like
cell shrinkage, nuclear condensation, DNA
fragmentation, and annexin V binding. Also, cell cycle
arrest at G1 phase, alteration of caspase-3, caspase-
9, Bcl-2 and PARP levels, loss of mitochondrial
membrane potential, and enhanced level of cytosolic
cytochrome c were observed in treated B16F10 cells.
Treatment with multiple doses of P(3a) significantly
increased the survival rate of B16F10 tumor bearing
BALB/c mice by suppressing the volume of tumor
while decreasing microvascular density and mitotic
index of the tumor cells