Category: 85953-29-3

Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors was written by Zhao, Bin;Li, Yixuan;Xu, Pan;Dai, Yang;Luo, Cheng;Sun, Yiming;Ai, Jing;Geng, Meiyu;Duan, Wenhu. And the article was included in ACS Medicinal Chemistry Letters in 2016.Computed Properties of C8H6ClFO2 This article mentions the following:

Fibroblast growth factor receptors (FGFRs) are important targets for cancer therapy. Herein, we describe the design, synthesis, and biol. evaluation of a novel series of 1H-pyrazolo[3,4-b]pyridine derivatives as potent and selective FGFR kinase inhibitors. On the basis of its excellent in vitro potency and favorable pharmacokinetic properties, compound I was selected for in vivo evaluation and showed significant antitumor activity in a FGFR1-driven H1581 xenograft model. These results indicated that I would be a promising candidate for further drug development. In the experiment, the researchers used many compounds, for example, Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3Computed Properties of C8H6ClFO2).

Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Computed Properties of C8H6ClFO2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors: Optimization of Whole-Cell Anticryptococcal Activity and Insights into the Structural Origins of Cryptococcal Selectivity was written by Marcyk, Paul T.;LeBlanc, Emmanuelle V.;Kuntz, Douglas A.;Xue, Alice;Ortiz, Francisco;Trilles, Richard;Bengtson, Stephen;Kenney, Tristan M. G.;Huang, David S.;Robbins, Nicole;Williams, Noelle S.;Krysan, Damian J.;Prive, Gilbert G.;Whitesell, Luke;Cowen, Leah E.;Brown, Lauren E.. And the article was included in Journal of Medicinal Chemistry in 2021.Synthetic Route of C8H6ClFO2 This article mentions the following:

The essential eukaryotic chaperone Hsp90 regulates the form and function of diverse client proteins, many of which govern thermotolerance, virulence, and drug resistance in fungal species. However, use of Hsp90 inhibitors as antifungal therapeutics has been precluded by human host toxicities and suppression of immune responses. We recently described resorcylate aminopyrazoles (RAPs) as the first class of Hsp90 inhibitors capable of discriminating between fungal (Cryptococcus neoformans, Candida albicans) and human isoforms of Hsp90 in biochem. assays. Here, we report an iterative structure-property optimization toward RAPs capable of inhibiting C. neoformans growth in culture. In addition, we report the first X-ray crystal structures of C. neoformans Hsp90 nucleotide binding domain (NBD), as the apoprotein and in complexes with the non-species-selective Hsp90 inhibitor NVP-AUY922 and three RAPs revealing unique ligand-induced conformational rearrangements, which reaffirm the hypothesis that intrinsic differences in protein flexibility can confer selective inhibition of fungal vs. human Hsp90 isoforms. In the experiment, the researchers used many compounds, for example, Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3Synthetic Route of C8H6ClFO2).

Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.Synthetic Route of C8H6ClFO2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Novel spirosuccinimides with incorporated isoindolone and benzisothiazole 1,1-dioxide moieties as aldose reductase inhibitors and antihyperglycemic agents was written by Wrobel, Jay;Dietrich, Arlene;Woolson, Shiela A.;Millen, Jane;McCaleb, Michael;Harrison, Maria C.;Hohman, Thomas C.;Sredy, Janet;Sullivan, Donald. And the article was included in Journal of Medicinal Chemistry in 1992.Computed Properties of C8H6ClFO2 This article mentions the following:

Compounds from two novel series of spirosuccinimides were prepared Analogs I (R = alkyl, aralkyl; R¹ = H, 4-, 5-, 6-, 7-Cl, 5,6-Cl₂, 6-F, 5-Br, 4-, 5-Me, 6-Co₂Me, 5,6-benzo, 5-Ph, 5-MeO, 5-MeS, 6-O₂N) possessed a spiro-fused isoindolone moiety while analogs II (R = alkyl, aralkyl) contained a spiro-fused benzisothiazole S,S-dioxide group. I and II were evaluated as aldose reductase inhibitors (ARI) in vitro by their ability to inhibit glyceraldehyde reduction using a partially purified bovine lens aldose reductase preparation and in vivo as inhibitors of galactitol accumulation in the lens, sciatic nerve, and diaphragm of galactose-fed rats. Many members from the isoindolone series I, particularly those with R = Me, showed good in vitro and in vivo potency. The most potent member, I (R = Me, R¹ = 6-Cl) (III), was resolved, and aldose reductase activity was found to reside almost exclusively in the (+)-enantiomer. III was approx. equipotent in the sciatic nerve of the galactose-fed rat to other cyclic imide ARI’s of similar in vitro activity, namely sorbinil and ADN-138 and also to tolrestat, an acetic acid-based ARI (ED₅₀ = 4-8 mg/kg). Compounds from both series I and II also lower plasma glucose levels of genetically obese db/db and ob/ob mice with potency similar to that of ciglitazone. However, members from these series failed to lower insulin levels of the ob/ob mouse at the doses tested. In the experiment, the researchers used many compounds, for example, Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3Computed Properties of C8H6ClFO2).

Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Computed Properties of C8H6ClFO2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

A new air-stable Si,S-chelating ligand for Ir-catalyzed directed ortho C-H borylation was written by Jiao, Jiao;Nie, Wenzheng;Song, Peidong;Li, Pengfei. And the article was included in Organic & Biomolecular Chemistry in 2021.Product Details of 85953-29-3 This article mentions the following:

A new air-stable Si,S-chelating ligand 1-(ⁱPrS)-2-(ⁱPr₂SiH)C₆H₄ (HL) has been developed and used in a directed ortho C-H borylation reaction of aromatic and heterocyclic compounds with B₂pin₂ catalyzed by [Ir(OMe)(cod)]₂/HL combination with a broad substrate scope, providing o-boryl-substituted aromatic and heterocyclic esters, amides and amines. This study provides the first example of using a sulfur-containing ligand in the catalytic C-H borylation process. It provides a rapid, efficient, and economical method for the preparation of organoboron compounds In the experiment, the researchers used many compounds, for example, Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3Product Details of 85953-29-3).

Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Product Details of 85953-29-3

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Novel Design of Nonpeptide AVP V₂ Receptor Agonists: Structural Requirements for an Agonist Having 1-(4-Aminobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepine as a Template was written by Kondo, Kazumi;Ogawa, Hidenori;Shinohara, Tomoichi;Kurimura, Muneaki;Tanada, Yoshihisa;Kan, Keizo;Yamashita, Hiroshi;Nakamura, Shigeki;Hirano, Takahiro;Yamamura, Yoshitaka;Mori, Toyoki;Tominaga, Michiaki;Itai, Akiko. And the article was included in Journal of Medicinal Chemistry in 2000.COA of Formula: C8H6ClFO2 This article mentions the following:

The discovery of a series of nonpeptide arginine vasopressin V₂ receptor agonists is described. After identifying the aniline derivative (I) as our lead compound from the metabolites of a previously studied compound that showed antidiuretic activity by po administration to Brattleboro rats, improvements in the in vitro potency involving evaluations of the structural requirements for agonist action and optimizing the structure of the benzoyl moiety have been intensively undertaken. These studies led to a series of compounds e.g. (II) that show potent agonist activity for the V₂ receptor. In the experiment, the researchers used many compounds, for example, Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3COA of Formula: C8H6ClFO2).

Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.COA of Formula: C8H6ClFO2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics