Isolation, structural elucidation and synthesis of novel antineoplastic substances denominated "combretastatins"
First Claim
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1. A substantially pure substance having the structure of either:
- ##STR6## wherein;
R1 is OH or OCH3 and R2 is H or OCH3 or R1 R2 is --OCH2 O--, R3 is H or OH, and R4 is OH or OCH3, with the proviso that when structure (I) is selected and R1 is OCH3, R2 is OCH3, R3 is OH and R4 is OCH3 ; and
that when structure (I) is selected and R1 R2 is --OCH2 O--, R3 is H and R4 is OCH3 ; and
that when structure (I) is selected and R1 is OH, R2 is OCH3, R3 is H and R4 is OCH3 ; and
that when structure (II) is selected and R4 is OH, R1 is OCH3, R2 is H or OCH3 and R3 is H; and
that when structure (II) is selected and R1 =R2 =OCH3, R3 is OH and R2 is OCH3 ; and
that when structure (II) is selected and R3 is OH, R4 is OCH3, R3 is H and R4 is OCH3.
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Abstract
New antineoplastic substances have been isolated, structurally elucidated and synthesized having a general structural formula of: ##STR1## wherein: R1 is OH or OCH3 ;
R2 is H or OCH3 ; or R1 R2 is --OCH2 O--;
R3 is H or OH; and
R4 is OH or OCH3.
These substances have been denominated "combretastatin A-1, -A-2, -A-3, -B-1, -B-2, -B-3 and -B-4". preparation containing the substances and methods of treating a host inflicted with a neoplastic growth with the preparation is described.
75 Citations
14 Claims
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1. A substantially pure substance having the structure of either:
- ##STR6## wherein;
R1 is OH or OCH3 and R2 is H or OCH3 or R1 R2 is --OCH2 O--, R3 is H or OH, and R4 is OH or OCH3, with the proviso that when structure (I) is selected and R1 is OCH3, R2 is OCH3, R3 is OH and R4 is OCH3 ; and
that when structure (I) is selected and R1 R2 is --OCH2 O--, R3 is H and R4 is OCH3 ; and
that when structure (I) is selected and R1 is OH, R2 is OCH3, R3 is H and R4 is OCH3 ; and
that when structure (II) is selected and R4 is OH, R1 is OCH3, R2 is H or OCH3 and R3 is H; and
that when structure (II) is selected and R1 =R2 =OCH3, R3 is OH and R2 is OCH3 ; and
that when structure (II) is selected and R3 is OH, R4 is OCH3, R3 is H and R4 is OCH3. - View Dependent Claims (2, 3, 4, 5, 6, 7)
- ##STR6## wherein;
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8. A pharmaceutical preparation comprising a pharmaceutically acceptable carrier and containing as its essential ingredient a synthesized substance having the structure of either:
- ##STR7## wherein;
R1 is OH or OCH3 and R2 is H or OCH3 or R1 R2 is --OCH2 O--, R3 is H or OH, and R4 is OH or OCH3, with the proviso that when structure (I) is selected and R1 is OCH3, R2 is OCH3, R3 is OH and R4 is OCH3 ; and
that when structure (I) is selected and R1 R2 is --OCH2 O--, R3 is H and R4 is OCH3 ; and
that when structure (I) is selected and R1 is OH, R2 is OCH3, R3 is H and R4 is OCH3 ; and
that when structure (II) is selected and R4 is OH, R1 is OCH3, R2 is H or OCH3 and R2 is H; and
that when structure (II) is selected and R1 =R2 =OCH3, R3 is OH and R4 is OCH3 ; and
that when structure (II) is selected and R1 is OH, R2 is OCH3, R3 is H and R4 is OCH3. - View Dependent Claims (9, 10, 11, 12, 13, 14)
- ##STR7## wherein;
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Current AssigneeArizona Board of Regents (University of Arizona)
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Original AssigneeArizona Board of Regents (University of Arizona)
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InventorsSingh, Sheo B., Pettit, George R.
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Primary Examiner(s)Raymond, Richard L.
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Assistant Examiner(s)LAMBKIN, DEBORAH C
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Application NumberUS08/340,156Time in Patent Office714 DaysField of Search568/646, 568/631, 514/720, 514/721, 514/464, 549/437US Class Current568/646CPC Class CodesA61P 35/00 Antineoplastic agentsC07C 43/23 containing hydroxy or O-met...C07D 317/64 Oxygen atoms
