EFFICACY OF 6-DIAZO-5-OXO-L-NORLEUCINE AND N-[N-GAMMA-GLUTAMYL-6-DIAZO-5-OXO-NORLEUCINYL]-6-DIAZO-5-OXO-NORLEUCINE AGAINST EXPERIMENTAL-TUMORS IN CONVENTIONAL AND NUDE-MICE

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  • 1 January 1979
    • journal article
    • research article
    • Vol. 39  (8) , 3220-3224
Abstract
The chemotherapeutic effects of 6-diazo-5-oxo-L-norleucine (DON) and N-[N-.gamma.-glutamyl-6-diazo-5-oxo-norleucinyl]-6-diazo-5-oxo-norleucine (azotomycin) were evaluated in a spectrum of transplantable experimental tumor systems including xenografts of human tumors in athymic mice. Both drugs displayed remarkable activity against murine leukemias L1210 and P388, colon tumors C26 and C38 and the CD8F1 mammary tumor. No significant activity was observed against Lewis lung carcinoma, B16 melanoma, and intracranial ependymoblastoma. DON and azotomycin exhibited striking inhibitory effects on the growth of s.c. human tumor (MX-1 mammary, LX-1 lung and CX-1 and CX-2 colon) xenografts in athymic mice. With the exception of 1 colon xenograft (CX-1), all tumor lines were markedly responsive to both drugs. Tumor regressions below the initial tumor sizes of 100-300 mg, albeit temporary, were brought about by 1 course of treatment every 4 days for 3 doses (at optimal dose) with either drug. Although these drugs were tested previously in the clinic and showed only limited therapeutic effectiveness, they seem worthy of a 2nd and closer look in light of recent laboratory results.