Ortho-quinone derivatives novel synthesis therefor and their use in the inhibition of neoplastic cell growth
First Claim
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1. A compound of Formula II:
- ##STR27## wherein R5 and R6 are each, independently, selected from the group consisting of H, C1 -C6 alkyl, C1 -C6 alkenyl, C1 -C6 alkoxy, C1 -C6 alkoxycarbonyl, --(CH2)n -aryl, and --(CH2)n -phenyl; and
R7 is selected from the group consisting of --(CH2)n -amino, β
-alanyl, malonyl, --(CH2)n -aryl, and --(CH2)n -phenyl, and n is an integer of from 0 to 10, and salts thereof.
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Abstract
The invention relates to β-lapachone derivatives of formula II and compositions containing said compounds: ##STR1## wherein, R5, R6 and R7 are as defined in the specification. The compounds are potent inhibitors of neoplastic cell growth and proliferation.
50 Citations
7 Claims
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1. A compound of Formula II:
- ##STR27## wherein R5 and R6 are each, independently, selected from the group consisting of H, C1 -C6 alkyl, C1 -C6 alkenyl, C1 -C6 alkoxy, C1 -C6 alkoxycarbonyl, --(CH2)n -aryl, and --(CH2)n -phenyl; and
R7 is selected from the group consisting of --(CH2)n -amino, β
-alanyl, malonyl, --(CH2)n -aryl, and --(CH2)n -phenyl, and n is an integer of from 0 to 10, and salts thereof. - View Dependent Claims (2)
- ##STR27## wherein R5 and R6 are each, independently, selected from the group consisting of H, C1 -C6 alkyl, C1 -C6 alkenyl, C1 -C6 alkoxy, C1 -C6 alkoxycarbonyl, --(CH2)n -aryl, and --(CH2)n -phenyl; and
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3. A pharmaceutical unit dosage form comprising an amount of a compound of Formula II:
- ##STR28## wherein R5 and R6 are each, independently, selected from the group consisting of H, C1 -C6 alkyl, C1 -C6 alkenyl, C1 -C6 alkoxy, C1 -C6 alkoxycarbonyl, --(CH2)n -aryl, and --(CH2)n -phenyl; and
R7 is selected from the group consisting of --(CH2)n -amino, β
-alanyl, malonyl, --(CH2)n -aryl, and --(CH2)n -phenyl, and wherein n is an integer of from 0 to 10;
pharmaceutically-suitable salts thereof, and combinations thereof; andwherein the amount is effective to inhibit growth of cancer cells in a human cancer patient following administration thereto. - View Dependent Claims (4, 5, 6, 7)
- ##STR28## wherein R5 and R6 are each, independently, selected from the group consisting of H, C1 -C6 alkyl, C1 -C6 alkenyl, C1 -C6 alkoxy, C1 -C6 alkoxycarbonyl, --(CH2)n -aryl, and --(CH2)n -phenyl; and
Specification
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Current AssigneeWisconsin Alumni Research Foundation (University of Wisconsin System)
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Original AssigneeWisconsin Alumni Research Foundation (University of Wisconsin System)
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InventorsSun, Jerry Shunneng, Geiser, Andrew H., Witiak, Donald T., Frydman, Benjamin J.
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Primary Examiner(s)Dees, Jose G.
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Assistant Examiner(s)BADIO, BARBARA P
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Application NumberUS08/604,131Time in Patent Office973 DaysField of Search549/389, 549/458, 549/454US Class Current514/454CPC Class CodesA61K 31/122 having the oxygen directly ...A61K 31/135 having aromatic rings , e.g...A61K 31/336 having three-membered rings...A61K 31/343 condensed with a carbocycli...A61K 31/352 condensed with carbocyclic ...C07C 323/22 containing thio groups and ...C07C 46/00 Preparation of quinonesC07C 50/32 the quinoid structure being...C07D 307/92 Naphthofurans; Hydrogenated...C07D 311/92 Naphthopyrans; Hydrogenated...
