A5107248950- Traditional and Medicinal Uses of Annonaceae
- Carbohydrate Chemistry and Synthesis
- Chemical Synthesis and Analysis
- PI3K/AKT/mTOR signaling in cancer
- Chronic Lymphocytic Leukemia Research
- Cocoa and Sweet Potato Agronomy
- Asymmetric Synthesis and Catalysis
- Cyclopropane Reaction Mechanisms
- Cytokine Signaling Pathways and Interactions
- Retinoids in leukemia and cellular processes
- Psoriasis: Treatment and Pathogenesis
- Advanced Synthetic Organic Chemistry
- Synthesis and Characterization of Heterocyclic Compounds
- Protein Kinase Regulation and GTPase Signaling
- Sexual Differentiation and Disorders
- Catalytic C–H Functionalization Methods
- Hormonal and reproductive studies
- Coenzyme Q10 studies and effects
- Vitamin D Research Studies
- Spam and Phishing Detection
- Catalytic Cross-Coupling Reactions
- Biochemical and Structural Characterization
- Sphingolipid Metabolism and Signaling
- Synthesis and Reactivity of Heterocycles
- Blood Coagulation and Thrombosis Mechanisms
Bristol-Myers Squibb (United States)
2005-2021
Bristol-Myers Squibb (Germany)
2008
Analytical Services
2005
Hunter College
1995-2002
γ-Lactams form important structural cores of a range medicinally relevant natural products and clinical drugs, principal examples being the new generation immunomodulatory imide drugs (IMiDs) brivaracetam family. Compared to conventional multistep synthesis, an intramolecular γ-C–H amination aliphatic amides would allow for direct construction valuable γ-lactam motifs from abundant amino acid precursors. Herein we report novel 2-pyridone ligand enabled Pd(II)-catalyzed γ-C(sp3)–H...
The trisubstituted pyrimidine 1 was identified through high-throughput screening as a novel calcium-sensing receptor (CaSR) antagonist. Small molecule CaSR antagonists and/or negative allosteric modulators have the potential to act an anabolic agent for treatment of osteoporosis. investigation structure−activity relationships around resulted in identification 18c and 18d, which showed efficacy at promoting PTH release vivo exhibited improved potency solubility over original lead 1.
PI3Kδ plays an important role controlling immune cell function and has therefore been identified as a potential target for the treatment of immunological disorders. This article highlights our work toward identification potent, selective, efficacious inhibitor. Through careful SAR, successful replacement polar pyrazole group by simple chloro or trifluoromethyl led to improved Caco-2 permeability, reduced efflux, hERG PC activity, increased selectivity profile while maintaining potency in...
Endocrine therapy of prostate cancer (PCa) relies on agents which disrupt the biosynthesis testosterone in testis and/or by direct antagonism active hormone androgen receptor (AR) non-gonadal target tissues action such as prostate.In an effort to evaluate new therapies could inhibit gonadal or biosynthesis, we developed high throughput biochemical and cellular screening assays identify inhibitors 17beta-hydroxysteroid dehydrogenase type III (17beta-HSD3), enzyme catalyzing conversion...
An efficient method for the solid-supported synthesis of 5-N-alkylamino and 5-N-arylamino pyrazoles is described. This general mild utilizes readily accessible resin-immobilized beta-ketoamides 2 as starting materials preparation 1. Resin-immobilized beta-ketoamide, aryl-, or alkylhydazine Lawesson's reagent are suspended in a mixture THF/Py heated at 50-55 degrees C to give resin-bound 5-aminopyrazole, that liberated from solid support by treatment with TFA.
A G-Protein-coupled receptor-targeted library of aryloxypropanolamines and aryloxybutanolamines was efficiently executed using a novel, polymer-supported acyclic acetal linker, producing compounds in good yields purities.
Abstract The chromosome 9p21 (chr9p21) locus is deleted in almost 10% of all cancer types. This includes the CDKN2A gene that encodes critical tumor suppressors p19-ARF and p16-INK4a. Methylthioadenosine phosphorylase (MTAP), a proximal to CDKN2A, co-deleted 80%-90% tumors with deletion. MTAP plays role methionine salvage pathway, deletion results accumulation its substrate methythioadenosine (MTA). Accumulation MTA partially inhibits activity arginine methyltransferase PRMT5, causing...
The direct conversion of solid-supported carboxylic acid allyl esters to carboxamides through the use phenylsilane and catalytic Pd under mild reaction conditions is reported. this methodology for generation a 48 compound solid-phase array described herein.