Abstract: Described are new 1-aziridino-1-hydroxyiminomethyl derivatives with the general formula (I), wherein R is able to is a single bond or a linker moiety capable of covalently bonding two aziridine oxime groups, R1 and R2 independently of one another are selected from the group consisting of —H, —CH3, —C2H5, —CN, —COOH, —COOCH3, —COOC2H5, —CONH2, or —C6H5 group, and n is the whole number 2, provided that R1 and R2 are not both —H and provided that R1 is not —H if R2 is —CH3 and R1 is not —CH3 if R2 is —H The compounds of general formula (I) show antitumor activity.
Abstract: The present invention relates to a novel benzoquinone, 2,5-diaziridinyl-3-(hydroxymethyl)-6-methyl-1,4-benzoquinone and its esters. The compounds can be used to treat tumors exhibiting elevated levels of the enzyme DT-diaphorase.
Type:
Grant
Filed:
May 24, 1999
Date of Patent:
December 5, 2000
Assignees:
Cancer Research Campaign Tech (London), University Technology Corp., University of Salford
Inventors:
David Ross, John Butler, Robert H. J. Hargreaves, David Siegel, Howard D. Beall
Abstract: The compounds of the formula: ##STR1## wherein R is selected from the group consisting of: (a) a substituent having the formula: ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen and --NO.sub.2,(b) a substituent having the formula: ##STR3## wherein R.sub.4 is hydrogen or an N(R').sub.2 substituent, wherein R' is an alkyl of 1 to 4 carbon atoms and R.sub.5 is CH or N,(c) alkyl of 1 to 18 carbon atoms,(d) halo-substituted alkyl of 1 to 6 carbon atoms,(e) styrenyl,(f) toluenyl, or(g) camphoryl.The compounds have been found to have anti-neoplastic activity for use in inhibiting the growth of tumors.