Synthesis and antileukemic activity of new 3-(5-methylisoxazol-3-yl) and 3-(pyrimidin-2-yl)-2-styrylquinazolin-4(3H)-ones.
3-(3-Methylisoxazol-5-yl) and 3-(pyrimidin-2-yl)-2-styrylquinazolin-4(3H)-ones 8a-l and 9a,c-e,h-l were synthesized by refluxing in acetic acid the corresponding 2-methylquinazolinones 6 and 8 with the opportune benzoic aldehyde for 12 h. The synthesized styrylquinazolinones 8a-l and 9a,c-e,h-l were tested in vitro for their antileukemic activity against L-1210 (murine leukemia), K-562 (human chronic myelogenous leukemia) and HL-60 (human leukemia) cell lines showing in some cases good activity.
Raffa
Demetrio
D
Dipartimento di Chimica e Tecnologie Farmaceutiche, Università degli Studi di Palermo, Via Archirafi 32, Palermo 90123, Italy. demraffa@unipa.it
Daidone
Giuseppe
G
Maggio
Benedetta
B
Cascioferro
Stella
S
Plescia
Fabiana
F
Schillaci
Domenico
D
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use*; D003078:Colchicine / Q000494:pharmacology; D018153:Czech Republic; D004353:Drug Evaluation, Preclinical / Q000379:methods; D018922:HL-60 Cells; D006801:Humans; D020014:K562 Cells; D007939:Leukemia L1210; D015394:Molecular Structure; D010080:Oxazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use
C500990:3-(5-methylisoxazol-3-yl)-2-styrylquinazolin-4(3H)-one; D000970:Antineoplastic Agents; D010080:Oxazoles; D011799:Quinazolines; D003078:Colchicine