Abstract:
A series of chalcones (3a-c) was synthesized and cyclocondensed with
hydrazine hydrate, hydroxylamine, urea and thiourea to afford novel
pyrazoline (4a-c), (5a-c), isoxazoline (6), dihyrdopyrimidinone (7a, b) and
dihyrdopyrimidinethione (8a, b) derivativesrespectively. In addition, a new
barbiturate (9) and thiobarbiturate (10) derivatives were synthesized by
reaction of chalcone derivatives with barbituric and thiobarbituric acid. Also, the novel pyrazolyl chalcone (13) was synthesized, reacted with
hydrazine hydrate in ethanol and acetic acid respectively, to afford new
pyrazoline derivative (14) and its N-acetyl derivative (15). Twelve of the
synthesized derivatives were selected by NCI to be evaluated for their
antitumor activity by in-vitro disease-oriented human cellsscreening panel
assay. All the tested compounds exhibited a broad spectrum of antitumor
activity especially against renal cancer UO-31. Compound (5c)is considered
to be the most active member identified in thisstudy with a broad spectrum
of activity against most cell lines.
