Potential antitumor agents IX: synthesis and antitumor activity of two analogues of ketocaine.
The reaction between o-hydroxybutyrophenone and tris(2-chloroethyl)amine gave two analogues (II, V) of the well-known local anesthetic ketocaine (I). Compounds II and V showed interesting antitumor activity in mice implanted with Ehrlich ascites tumor cells (% T/C = 149 at 5 mg/kg and 171 at 50 mg/kg, respectively). Further studies on the pharmacological behavior of these new compounds are in progress.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002090:Butyrophenones / Q000138:chemical synthesis* / Q000494:pharmacology; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D005260:Female; D051379:Mice
D000970:Antineoplastic Agents; D002090:Butyrophenones