The mono- and di-methoxy substituted benzohydroxamic acids proved to be pot
ent antineoplastic/cytotoxic agents effectively suppressing growth in suspe
nded tumor cells and demonstrated some selectivity against certain human ca
rcinomas. These methoxy derivatives inhibited L1210 DNA and protein synthes
es. They were metabolic inhibitors of the activities of regulatory enzymes
of de novo purine and pyrimidine syntheses in L1210 lymphocytic leukemia ce
lls after 60 min at 100 mu M. Ribonucleoside reductase, dihydrofolate reduc
tase and DNA polymerase a activities were also moderately suppressed by the
se agents which would add to the overall reduction of DNA synthesis as well
as tumor cell growth.