Category: 1008506-24-8

Toure, B. Barry published the artcileToward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight, Product Details of C6H8BNO3, the publication is Journal of Medicinal Chemistry (2016), 59(10), 4711-4723, database is CAplus and MEDLINE.

MELK kinase has been implicated in playing an important role in tumorigenesis. Our previous studies suggested that MELK is involved in the regulation of cell cycle and its genetic depletion leads to growth inhibition in a subset of high MELK-expressing basal-like breast cancer cell lines. Herein we describe the discovery and optimization of novel MELK inhibitors 8a and 8b that recapitulate the cellular effects observed by short hairpin RNA (shRNA)-mediated MELK knockdown in cellular models. We also discovered a novel fluorine-induced hydrophobic collapse that locked the ligand in its bioactive conformation and led to a 20-fold gain in potency. These novel pharmacol. inhibitors achieved high exposure in vivo and were well tolerated, which may allow further in vivo evaluation.

Journal of Medicinal Chemistry published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C10H9NO4S, Product Details of C6H8BNO3.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Law, Robert P. published the artcileDiscovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain, Safety of 3-Methoxypyridine-4-boronic acid, the publication is Journal of Medicinal Chemistry (2018), 61(10), 4317-4334, database is CAplus and MEDLINE.

The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomains-BRD2, BRD3, BRD4, and BRDT-each contain two bromodomain modules. BET bromodomain inhibition is a potential therapy for various cancers and immunoinflammatory diseases, but few reported inhibitors show selectivity within the BET family. Inhibitors with selectivity for the first or second bromodomain are desired to aid investigation of the biol. function of these domains. Focused library screening identified a series of tetrahydroquinoxalines with selectivity for the second bromodomains of the BET family (BD2). Structure-guided optimization of the template improved potency, selectivity, and physicochem. properties, culminating in potent BET inhibitors with BD2 selectivity.

Journal of Medicinal Chemistry published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, Safety of 3-Methoxypyridine-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Vasbinder, Melissa M. published the artcileDiscovery and Optimization of a Novel Series of Potent Mutant B-Raf^V600E Selective Kinase Inhibitors, SDS of cas: 1008506-24-8, the publication is Journal of Medicinal Chemistry (2013), 56(5), 1996-2015, database is CAplus and MEDLINE.

B-Raf represents an attractive target for anticancer therapy, and the development of small mol. B-Raf inhibitors has delivered new therapies for metastatic melanoma patients. The authors have discovered a novel class of small mols. that inhibit mutant B-Raf^V600E kinase activity both in vitro and in vivo. Investigations into the structure-activity relationships of the series are presented along with efforts to improve upon the cellular potency, solubility, and pharmacokinetic profile. Compounds selectively inhibited B-Raf^V600E in vitro and showed preferential antiproliferative activity in mutant B-Raf^V600E cell lines and exhibited selectivity in a kinase panel against other kinases. Examples from this series inhibit growth of a B-Raf^V600E A375 xenograft in vivo at a well-tolerated dose. In addition, aminoquinazolines described herein were shown to display pERK elevation in nonmutant B-Raf cell lines in vitro.

Journal of Medicinal Chemistry published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C11H8O3, SDS of cas: 1008506-24-8.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem