Journal of Pharmaceutical Sciences p. 1175 - 1177 (1984)
Update date:2022-07-31
Topics:
Andreani
Bonazzi
Rambaldi
Galatulas
Bossa
The synthesis of two nitrogen mustard derivatives (VIII and IX) related to the well-known local anesthetic ketocaine (III) is reported. These compounds were tested in mice implanted with Ehrlich ascites tumor cells, and the antitumor activity was compared with that of two previously synthesized analogues (I and II) lacking the nitro group and with that of doxorubicin. The monofunctional compound IX was inactive, but the bifunctional compound VIII showed potent antitumor activity (%T/C > 254 at 20 mg/kg).
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(1964)