228 results on '"Borzilleri, Robert"'
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2. TGFβ2 and TGFβ3 mediate appropriate context-dependent phenotype of rat valvular interstitial cells
3. Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form
4. Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI)
5. Antibody–drug conjugates: current status and future directions
6. Long-Acting Tumor-Activated Prodrug of a TGFβR Inhibitor
7. Pharmacology of smac mimetics; chemotype differentiation based on physical association with caspase regulators and cellular transport
8. Mcl-1 antagonism is a potential therapeutic strategy in a subset of solid cancers
9. Assessing compound binding to the Eg5 motor domain using a thermal shift assay
10. Development of a Stereoselective and Scalable Synthesis for the Potent Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor, BMT-297376; N-((R)-1-((cis)-4-(3-(Difluoromethyl)-2-methoxypyridin-4-yl)cyclohexyl)propyl)-6-methoxynicotinamide
11. Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors
12. Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis
13. JAK Family Inhibitors for Autoimmune Diseases
14. Preclinical discovery of ixabepilone, a highly active antineoplastic agent
15. Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy
16. Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1
17. Pharmacodynamics‐based approach for efficacious human dose projection of BMS‐986260, a small molecule transforming growth factor beta receptor 1 inhibitor
18. Design, Synthesis, and Structure–Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody–Drug Conjugates
19. Chapter 15 Case History: Discovery of Ixabepilone (IXEMPRATM), a First-in-Class Epothilone Analog for Treatment of Metastatic Breast Cancer
20. Development of a Scalable Synthesis of the Small Molecule TGFβR1 Inhibitor BMS-986260
21. Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent
22. A novel application of a Pd(0)-catalyzed nucleophilic substitution reaction to the regio- and stereoselective synthesis of lactam analogues of the epothilone natural products
23. Synthesis of the vancomycin CD and DE ring systems
24. Synthesis of (9R, 12S)- and (S, 12S)-cycloisodityrosine and their N-methyl derivatives
25. Highly Efficient Semisynthesis of Biologically Active Epothilone Derivatives
26. Synthesis of (R)-(4-methoxy-3,5-dihydroxyphenyl)glycine derivatives: the central amino acid of vancomycin and related agents
27. Total synthesis of the unusual marine alkaloid (-)-papuamine utilizing a novel imino ene reaction
28. Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads
29. Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents
30. Discovery of tetrahydroisoquinoline-based bivalent heterodimeric IAP antagonists
31. Decarboxylative Peptide Macrocyclization through Photoredox Catalysis
32. DGKα/ζ inhibitors combine with PD-1 checkpoint therapy to promote T cell–mediated antitumor immunity
33. Building homogeneous time-resolved fluorescence resonance energy transfer assays for characterization of bivalent inhibitors of an inhibitor of apoptosis protein target
34. Ultrasensitive Quantitative LC–MS/MS of an Inhibitor of Apoptosis Protein’s Antagonist in Plasma Using Protein Target Affinity Extraction
35. Antroquinonol A: Scalable Synthesis and Preclinical Biology of a Phase 2 Drug Candidate
36. Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists
37. Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists
38. Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer
39. The Discovery of Macrocyclic XIAP Antagonists from a DNA-Programmed Chemistry Library, and Their Optimization To Give Lead Compounds with in Vivo Antitumor Activity
40. Discovery of Potent Heterodimeric Antagonists of Inhibitor of Apoptosis Proteins (IAPs) with Sustained Antitumor Activity
41. Decarboxylative Peptide Macrocyclization through Photoredox Catalysis.
42. Design, synthesis and structure–activity relationships of novel biarylamine-based Met kinase inhibitors
43. Total synthesis of papuamine via stereospecific intramolecular imino ene reaction of an allenylsilane
44. beta-Tosylethylamine: a useful reagent for preparation of N-protected amides, carbamates, and related compounds. Application to synthesis of beta-lactams
45. Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors
46. Identification of pyrrolo[2,1- f][1,2,4]triazine-based inhibitors of Met kinase
47. Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1- f][1,2,4]triazine-based VEGFR-2 kinase inhibitors
48. Cytochrome P450 11A1 Bioactivation of a Kinase Inhibitor in Rats: Use of Radioprofiling, Modulation of Metabolism, and Adrenocortical Cell Lines to Evaluate Adrenal Toxicity
49. ChemInform Abstract: Synthesis and Biological Activity of Novel Epothilone Aziridines.
50. Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily
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