- POTENT SMALL MOLECULE INHIBITORS OF AUTOPHAGY, AND METHODS OF USE THEREOF
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Certain aspects of the invention relate to small molecule autophagy inhibitors, and their use for treatment and prevention of cancers and acute pancreatitis. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity.
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- Anticoagulant contrast media
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The present invention provides novel anticoagulant contrast agents, which comprise an organic scaffolding moiety, an organic anticoagulant moiety, and an imaging moiety. The invention also provides anticoagulant contrast media and methods of visualizing internal structures utilizing the novel anticoagulant contrast agents and anticoagulant contrast media.
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Page/Page column 19-20
(2010/02/15)
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- Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics
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The design, synthesis and biological activity of non-covalent thrombin inhibitors incorporating 4,5,6,7-tetrahydroindazole, 2-methyl-4,5,6,7-tetrahydroindazole, 4,5,6,7-tetrahydroisoindole, 5,6,7,8-tetrahydroquinazoline and 5,6,7,8-tetrahydroquinazolin-2-amine as novel, partially saturated, heterobicyclic P1-arginine side-chain mimetics is described. The binding mode of the most potent candidate in the series co-crystallized with human α-thrombin, which exhibited an in vitro Ki of 140 nM and more that 478-fold selectivity against trypsin, is discussed.
- Peterlin-Masic, Lucija,Mlinsek, Gregor,Solmajer, Tomaz,Trampus-Bakija, Alenka,Stegnar, Mojca,Kikelj, Danijel
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p. 789 - 794
(2007/10/03)
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- Bicyclic and tricyclic ergoline partial structures: Rigid 3-(2-aminoethyl)pyrroles and 3- and 4-(2-aminoethyl)pyrazoles as dopamine agonists
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It is proposed, based upon comparisons with apomorphine, that the rigid pyrroleethylamine moiety of the ergolines is the portion of the molecule responsible for dopamine agonist activity. In support of this hypothesis, bicyclic and tricyclic ergoline part
- Bach,Kornfeld,Jones,Chaney,Dorman,Paschal,Clemens,Smalstig
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p. 481 - 491
(2007/10/02)
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