47 results on '"Dakin, Les A."'
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2. AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia
3. Synthesis of the C1-C11' oxazole-containing side chain of leucascandrolide A. Application of a Sonogashira cross-coupling
4. Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254)
5. Lewis acid-mediated carbocyclization reactions to chiral (E)-crotylsilanes
6. Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases
7. Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas
8. Discovery, design, and synthesis of indole-based EZH2 inhibitors
9. [4+2]-Annulations of chiral organosilanes: Application to the total synthesis of leucascandrolide A
10. Synthesis of PF-06928215 and analogues v1
11. Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507
12. Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains
13. Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases
14. Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO
15. 3-Amido-4-anilinocinnolines as a novel class of CSF-1R inhibitor
16. Abstract 5526: Inhibition of the histone methyl transferase EZH2 causes viability defects in multiple myeloma
17. A Practical Synthesis of Indoles via a Pd-Catalyzed C–N Ring Formation
18. 3-Amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile
19. Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity
20. Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)
21. Abstract 2353: Novel inhibitors of PIM-1, PIM-2, and PIM-3 protein kinases: medicinal chemistry leading to AZD1208.
22. Abstract 4621: The histone methyltransferase EZH2 catalytic activity is required for cell growth in diffuse large B-cell lymphoma.
23. Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer
24. Abstract 2796: Efficacy and biomarker modulation by AZD1208, a novel, potent and selective pan-Pim kinase inhibitor, in models of acute myeloid leukemia
25. AZD1208, a Novel, Potent and Selective Pan PIM Kinase Inhibitor, Demonstrates Efficacy in Models of Acute Myeloid Leukemia
26. ChemInform Abstract: Carbenoid Insertions into the Silicon-Hydrogen Bond Catalyzed by Chiral Copper(I) Schiff Base Complexes.
27. [4 + 2]-Annulations of Chiral Organosilanes: Application to the Total Synthesis of Leucascandrolide A (I).
28. Slow-Onset, Long-Duration, Alkyl Analogues of Methylphenidate with Enhanced Selectivity for the Dopamine Transporter
29. [4 + 2]-Annulations of Chiral Organosilanes: Application to the Total Synthesis of Leucascandrolide A
30. Vinylogous amide analogs of methylphenidate
31. Enantioselective [4 + 2]-Annulation of Chiral Crotylsilanes: Application to the Synthesis of a C1−C22 Fragment of Leucascandrolide A
32. A Mild, Chemoselective Protocol for the Removal of Thioketals and Thioacetals Mediated by Dess—Martin Periodinane.
33. A Mild, Chemoselective Protocol for the Removal of Thioketals and Thioacetals Mediated by Dess−Martin Periodinane
34. Sonogashira Coupling of Functionalized Trifloyl Oxazoles and Thiazoles with Terminal Alkynes: Synthesis of Disubstituted Heterocycles.
35. Synthesis of the C1‘−C11‘ Oxazole-Containing Side Chain of Leucascandrolide A. Application of a Sonogashira Cross-Coupling
36. Speciation and Mechanistic Studies of Chiral Copper(I) Schiff Base Precursors Mediating Asymmetric Carbenoid Insertion Reactions of Diazoacetates into the Si−H Bond of Silanes
37. A Practical Synthesis of Indoles via a Pd-CatalyzedC–N Ring Formation.
38. Carbenoid insertions into the siliconhydrogen bond catalyzed by chiral copper (I) schiff base complexes
39. Lewis Acid-Mediated Carbocyclization Reactions of Chiral (E)-Crotylsilanes
40. Structure-and Reactivity-Based Development of CovalentInhibitors of the Activating and Gatekeeper Mutant Forms of the EpidermalGrowth Factor Receptor (EGFR).
41. [4 + 2]-Annulations of Chiral Organosilanes: Application to the Total Synthesis of Leucascandrolide A.
42. ChemInform Abstract: Carbenoid Insertions into the Silicon-Hydrogen Bond Catalyzed by Chiral Copper(I) Schiff Base Complexes.
43. Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
44. [4 + 2]-annulations of chiral organosilanes: Application to the total synthesis of leucascandrolide A.
45. Enantioselective [4 + 2]-annulation of chiral crotylsilanes: application to the synthesis of a C1-C22 fragment of leucascandrolide A.
46. A mild, chemoselective protocol for the removal of thioketals and thioacetals mediated by Dess-Martin periodinane.
47. Sonogashira coupling of functionalized trifloyl oxazoles and thiazoles with terminal alkynes: synthesis of disubstituted heterocycles.
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