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Continued optimization of the M

Vanderbilt University School of Medicine

Development of thieno- and benzopyrimidinone inhibitors of the Hedgehog signaling pathway reveals PDE4-dependent and PDE4-independent mechanisms of action.

Vanderbilt University School of Medicine

Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.

Vanderbilt University School of Medicine

Inhibition of human DNA topoisomerase IIa by two novel ellipticine derivatives.

Vanderbilt University School of Medicine

Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design.

Vanderbilt University School of Medicine

Diphenylpyrazoles as replication protein a inhibitors.

Vanderbilt University School of Medicine

Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).

Vanderbilt University School of Medicine

Design of Fluorine-Containing 3,4-Diarylfuran-2(5H)-ones as Selective COX-1 Inhibitors.

Vanderbilt University School of Medicine

Fragment-based screening of the bromodomain of ATAD2.

Vanderbilt University School of Medicine

Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A.

Vanderbilt University School of Medicine

Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach.

Vanderbilt University School of Medicine

Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A.

Vanderbilt University School of Medicine

Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17ß-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.

Vanderbilt University School of Medicine

Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.

Vanderbilt University School of Medicine

Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere.

Vanderbilt University School of Medicine

Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.

Vanderbilt University School of Medicine

Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.

Vanderbilt University School of Medicine

Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.

Vanderbilt University School of Medicine

Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe.

Vanderbilt University School of Medicine

Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.

Vanderbilt University School of Medicine

Podophyllotoxin analogues active versus Trypanosoma brucei.

Vanderbilt University School of Medicine

The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives.

Vanderbilt University School of Medicine

Discovery of VU0467485/AZ13713945: An M

Vanderbilt University School of Medicine

Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.

Vanderbilt University School of Medicine

Fragment-Based Discovery of Small Molecules Bound to T-Cell Immunoglobulin and Mucin Domain-Containing Molecule 3 (TIM-3).

Vanderbilt University School of Medicine

Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M

Vanderbilt University School of Medicine

Harmaline Analogs as Substrate-Selective Cyclooxygenase-2 Inhibitors.

Vanderbilt University School of Medicine

Targeted Detection of Cyclooxygenase-1 in Ovarian Cancer.

Vanderbilt University School of Medicine

Enantiospecific, selective cyclooxygenase-2 inhibitors.

Vanderbilt University School of Medicine

Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.

Vanderbilt University School of Medicine

VU6005806/AZN-00016130, an advanced M

Vanderbilt University School of Medicine

Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods.

Vanderbilt University School of Medicine

Multistep Binding of the Non-Steroidal Inhibitors Orteronel and Seviteronel to Human Cytochrome P450 17A1 and Relevance to Inhibition of Enzyme Activity.

Vanderbilt University School of Medicine

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.

Vanderbilt University School of Medicine

Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.

Vanderbilt University School of Medicine

Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu

Vanderbilt University School of Medicine

Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.

Vanderbilt University School of Medicine

Validation of Human Sterol 14α-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors.

Vanderbilt University School of Medicine

Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu

Vanderbilt University School of Medicine

Design, synthesis, and biochemical evaluation of N-substituted maleimides as inhibitors of prostaglandin endoperoxide synthases.

Vanderbilt University School of Medicine

Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae.

Vanderbilt University School of Medicine

Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS.

Vanderbilt University School of Medicine

Challenges in the development of an M

Vanderbilt University School of Medicine

Design and Synthesis of

Vanderbilt University School of Medicine

Sterol 14α-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis.

Vanderbilt University School of Medicine

Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.

Vanderbilt University School of Medicine

Challenges in the development of an M

Vanderbilt University School of Medicine

Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.

Vanderbilt University School of Medicine

Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.

Vanderbilt University School of Medicine

Acetylcholinesterase inhibitors for potential use in Alzheimer's disease: molecular modeling, synthesis and kinetic evaluation of 11H-indeno-[1,2-b]-quinolin-10-ylamine derivatives.

University of Bologna