- 3,4-DISUBSTITUTED MALEIMIDES FOR USE AS VASCULAR DAMAGING AGENTS
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This invention relates to novel compounds of Formula (I) for use as vascular damaging agents: Formula (I) wherein Rl, R7, R8, R9, ARI, AR2, AR3, p, q and r are as described in the specification. The invention also relates to methods for preparing compounds of Formula (I), to their use as medicaments (including methods for the treatment of angiogenesis or disease states associated with angiogenesis) and to pharmaceutical compositions containing compounds of Formula (I).
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Page/Page column 59
(2008/06/13)
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- Design of Inhibitors from the Three-Dimensional Structure of Alcohol Dehydrogenase. Chemical Synthesis and Enzymatic Properties
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Inhibitors of liver alcohol dehydrogenase were designed from the three-dimensional structure of the enzyme.The ligand to the catalytic zinc ion is an amide group or, better, a formamide group.With the latter function, a hydrogen bond between the NH group and the hydroxyl group of Ser-48 may be formed.The hydrophobic substrate binding site brings structural restraints. α-ω bifunctional molecules show good inhibitory properties possibly due to the interactions with polar residues at the entrance of the substrate binding site.
- Freudenreich, Charles,Samama, Jean-Pierre,Biellmann, Jean-Francois
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p. 3344 - 3353
(2007/10/02)
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