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- W2187940233 abstract "SUMMARY 4-Methyl-5-amino-1-formylisoquinoline thiosemicarba zone (MAIQ-1) was studied to determine its potential for clinical trial as a second-generation antineoplastic agent of the a-(N)-heterocyclic camboxaldehydethiosemicambazone class. MAIQ-1 was shown to be among the most potent known inhibitors of the major target for the expression of antineoplastic activity by this class of agents, the enzyme nibonucleoside diphosphate neductase, requiring only 0.06 @M for 50% inhibition. This potency at the enzymatic level was consistent with its antineoplastic activity against the mumineneoplasms Sarcoma 180, Leukemia L1210, Leuke mia P388, and the B16 melanoma. The acetybationof the 5amino group of the model substrate 5-amino-i ,4-dimethyli soquinoline was lower than that of 5-amino-1-methylisoqui nobinewhen incubated with acetyl-coenzyme A and rat liver homogenate. This finding suggests that the presence of the 4-methyl function offers stenic hinderance to enzymatic substitution of the adjacent 5-amino group. In vivo metabo bism of MAIQ-1 in mice, studied with [3'-14C]MAIQ-i, showed that relatively slow excretion of this agent oc cummed, since the cumulative urinary excretion of madioactiv ity was only 35% in 48 hr. About 51% of excreted urinary radioactivity was present in chnomatognamsin an area con responding to @he iron chelate of MA1Q-i , and only a minor quantity of material migrating like acetylated MAIQ-1 was present in urine, a finding consistent with enzymatic data with liver homogenates. The results indicate that MAIQ-i has the antineoplastic activity, enzyme inhibitory potency, and relative resistance to metabolic inactivation required of an agent of this class for clinical trials." @default.
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- W2187940233 date "1977-01-01" @default.
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- W2187940233 title "4-Methyl-5-amino-1 -formylisoquinolineThiosemicarbazone, a Second-GenerationAntineoplasticAgent of the a-(N) HeterocyclicCarboxaldehydeThiosemicarbazoneSeries1" @default.
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