Category: 766549-26-2

Kedari, Chaitanya Kumar published the artcileBiarylmethoxy Nicotinamides As Novel and Specific Inhibitors of Mycobacterium tuberculosis, Computed Properties of 766549-26-2, the publication is ACS Medicinal Chemistry Letters (2014), 5(5), 491-495, database is CAplus and MEDLINE.

A whole cell based screening effort on a focused library from corporate collection resulted in the identification of biarylmethoxy nicotinamides as novel inhibitors of M. tuberculosis (Mtu) H37Rv. The series exhibited tangible structure-activity relationships, and during hit to lead exploration, a cellular potency of 100 nM was achieved, which is an improvement of >200-fold from the starting point. The series is very specific to Mtu and noncytotoxic up to 250 μM as measured in the mammalian cell line THP-1 based cytotoxicity assay. This compound class retains its potency on several drug sensitive and single drug resistant clin. isolates, which indicate that the compounds could be acting through a novel mode of action.

ACS Medicinal Chemistry Letters published new progress about 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, Computed Properties of 766549-26-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Raimundo, Brian C. published the artcileIntegrating Fragment Assembly and Biophysical Methods in the Chemical Advancement of Small-Molecule Antagonists of IL-2: An Approach for Inhibiting Protein-Protein Interactions, Recommanded Product: 2-Chloro-4-hydroxyphenylboronic acid, the publication is Journal of Medicinal Chemistry (2004), 47(12), 3111-3130, database is CAplus and MEDLINE.

Fragment assembly has shown promise for discovering small-mol. antagonists for difficult targets, including protein-protein interactions. Here, the authors describe a process for identifying a 60 nM inhibitor of the interleukin-2 (IL-2)/IL-2 receptor (IL-2Rα) interaction. By use of fragment-based approaches, a compound with millimolar affinity was evolved to a hit series with low micromolar activity, and these compounds were optimized into a lead series with nanomolar affinity. Fragment assembly was useful not only for hit identification, but also for lead optimization. Throughout the discovery process, biophys. methods and structural biol. demonstrated that compounds bound reversibly to IL-2 at the IL-2 receptor binding site.

Journal of Medicinal Chemistry published new progress about 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, Recommanded Product: 2-Chloro-4-hydroxyphenylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Jansa, Josef published the artcileImidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure, Recommanded Product: 2-Chloro-4-hydroxyphenylboronic acid, the publication is European Journal of Medicinal Chemistry (2021), 113309, database is CAplus and MEDLINE.

Pharmacol. inhibition of cyclin-dependent kinases has emerged as a possible treatment option for various cancer types. Authors recently identified substituted imidazo[1,2-c]pyrimidin-5(6H)-ones as inhibitors of cyclin-dependent kinase 2 (CDK2). Here, the synthesis of derivatives modified at positions 2, 3, 6 or 8 prepared using Suzuki-Miyaura cross-coupling, halogenation, Dimroth-type rearrangement and alkylation as the main synthetic methods was reported. The compounds displayed micro- to submicromolar inhibition of CDK2/cyclin E activity. Binding of the most potent compound I to CDK2 was determined using isothermal titration calorimetry. The co-crystal structure of I in complex with fully active CDK2 was solved, revealing the binding mode of I in the ATP pocket and a hydrogen bonding interaction with hinge region residue Leu83. Evaluation against leukemia cell lines revealed low cytotoxicity, which is in line with the high selectivity towards CDK2. This study demonstrates that substituted imidazo[1,2-c]pyrimidines can be exploited for future kinase inhibitor development.

European Journal of Medicinal Chemistry published new progress about 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, Recommanded Product: 2-Chloro-4-hydroxyphenylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Lesuisse, Dominique published the artcileRational design of potent GSK3β inhibitors with selectivity for Cdk1 and Cdk2, SDS of cas: 766549-26-2, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(6), 1985-1989, database is CAplus and MEDLINE.

From an HTS hit, a series of potent and selective aminoindazole inhibitors of GSK3β have been designed based on a Cdk2-homol. model and with the help of several crystal structures of the compounds within Cdk2.

Bioorganic & Medicinal Chemistry Letters published new progress about 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, SDS of cas: 766549-26-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Shen, Hong C. published the artcileDiscovery of Biaryl Anthranilides as Full Agonists for the High Affinity Niacin Receptor, Product Details of C6H6BClO3, the publication is Journal of Medicinal Chemistry (2007), 50(25), 6303-6306, database is CAplus and MEDLINE.

Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintaining excellent receptor activity. Compound 2i (I) exhibited good in vivo antilipolytic efficacy while providing a significantly improved therapeutic index over vasodilation (flushing) with respect to niacin in the mouse model.

Journal of Medicinal Chemistry published new progress about 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C8H10O2, Product Details of C6H6BClO3.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics