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Synthesis and antitumor activity of some novel heterocyclic compounds derived from chalcone analogues

Manal M.Kandeel, Nadia A.Abdou, Hanan H.Kadry, Rana M.El-Masry

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) derivatives respectively. 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 cells screening panel assay. All the tested compounds exhibited a broad spectrum of antitumor activity especially against renal cancerUO-31. Compound (5c) is considered to be the most active member identified in this study with a broad spectrum of activity against most cell lines.