Category: 97009-67-1

Groen, Aaron C. published the artcileA novel small-molecule inhibitor reveals a possible role of kinesin-5 in anastral spindle-pole assembly, Formula: C10H8FN, the main research area is FCPT ATPase inhibitor kinesin spindle pole assembly.

The tetrameric plus-end-directed motor, kinesin-5, is essential for bipolar spindle assembly. Small-mol. inhibitors of kinesin-5 have been important tools for investigating its function, and some are currently under evaluation as anti-cancer drugs. Most inhibitors reported to date are ‘non-competitive’ and bind to a specific site on the motor head, trapping the motor in an ADP-bound state in which it has a weak but non-zero affinity for microtubules. Here, we used a novel ATP-competitive inhibitor, FCPT, developed at Merck (USA). We found that it induced tight binding of kinesin-5 onto microtubules in vitro. Using Xenopus egg-extract spindles, we found that FCPT not only blocked poleward microtubule sliding but also selectively induced loss of microtubules at the poles of bipolar spindles (and not asters or monoasters). We also found that the spindle-pole proteins TPX2 and γ-tubulin became redistributed to the spindle equator, suggesting that proper kinesin-5 function is required for pole assembly.

Journal of Cell Science published new progress about Centrosome. 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Formula: C10H8FN.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Huang, Adrian published the artcileDiscovery of 2-[1-(4-Chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic Acid (PSI-421), a P-Selectin Inhibitor with Improved Pharmacokinetic Properties and Oral Efficacy in Models of Vascular Injury, Related Products of nitriles-buliding-blocks, the main research area is quinoline preparation P selectin inhibitor SAR.

Previously, we reported the discovery of PSI-697 (1a), a C-2 benzyl substituted quinoline salicylic acid-based P-selectin inhibitor. It is active in a variety of animal models of cardiovascular disease. Compound 1a has also been shown to be well tolerated and safe in healthy volunteers at doses of up to 1200 mg in a phase 1 single ascending dose study. However, its oral bioavailability was low. Our goal was to identify a back up compound with equal potency, increased solubility, and increased exposure. We expanded our structure-activity studies in this series by branching at the α position of the C-2 benzyl side chain and through modification of substituents on the carboxylic A-ring of the quinoline. This resulted in discovery of PSI-421 with marked improvement in aqueous solubility and pharmacokinetic properties. This compound has shown oral efficacy in animal models of arterial and venous injury and was selected as a preclin. development compound for potential treatment of such diseases as atherosclerosis and deep vein thrombosis.

Journal of Medicinal Chemistry published new progress about Arterial injury. 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Related Products of nitriles-buliding-blocks.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Groen, Aaron C. published the artcileA novel small-molecule inhibitor reveals a possible role of kinesin-5 in anastral spindle-pole assembly, Formula: C10H8FN, the main research area is FCPT ATPase inhibitor kinesin spindle pole assembly.

The tetrameric plus-end-directed motor, kinesin-5, is essential for bipolar spindle assembly. Small-mol. inhibitors of kinesin-5 have been important tools for investigating its function, and some are currently under evaluation as anti-cancer drugs. Most inhibitors reported to date are ‘non-competitive’ and bind to a specific site on the motor head, trapping the motor in an ADP-bound state in which it has a weak but non-zero affinity for microtubules. Here, we used a novel ATP-competitive inhibitor, FCPT, developed at Merck (USA). We found that it induced tight binding of kinesin-5 onto microtubules in vitro. Using Xenopus egg-extract spindles, we found that FCPT not only blocked poleward microtubule sliding but also selectively induced loss of microtubules at the poles of bipolar spindles (and not asters or monoasters). We also found that the spindle-pole proteins TPX2 and γ-tubulin became redistributed to the spindle equator, suggesting that proper kinesin-5 function is required for pole assembly.

Journal of Cell Science published new progress about Centrosome. 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Formula: C10H8FN.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Tu, Hua published the artcileDistinctive molecular inhibition mechanisms for selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1, Quality Control of 97009-67-1, the main research area is sulfonamide triazole hydroxysteroid dehydrogenase inhibitor preparation; non insulin dependent diabetes antidiabetic hydroxysteroid dehydrogenase inhibitor.

11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the NADPH dependent interconversion of inactive cortisone to active cortisol. Excess 11β-HSD1 or cortisol leads to insulin resistance and metabolic syndrome in animal models and in humans. Inhibiting 11β-HSD1 activity signifies a promising therapeutic strategy in the treatment of Type 2 diabetes and related diseases. Herein, the authors report two highly potent and selective small mol. inhibitors of human 11β-HSD1. While compound (I), a sulfonamide, functions as a simple substrate competitive inhibitor, compound (II), a triazole, shows the kinetic profile of a mixed inhibitor. Co-crystal structures reveal that both compounds occupy the 11β-HSD1 catalytic site, but present distinct mol. interactions with the protein. Strikingly, compound (II) interacts much closer to the cofactor NADP+ and likely modifies its binding. Together, the structural and kinetic analyses demonstrate two distinctive mol. inhibition mechanisms, providing valuable information for future inhibitor design.

Bioorganic & Medicinal Chemistry published new progress about Antidiabetic agents. 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Quality Control of 97009-67-1.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Tu, Hua published the artcileDistinctive molecular inhibition mechanisms for selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1, Quality Control of 97009-67-1, the main research area is sulfonamide triazole hydroxysteroid dehydrogenase inhibitor preparation; non insulin dependent diabetes antidiabetic hydroxysteroid dehydrogenase inhibitor.

11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the NADPH dependent interconversion of inactive cortisone to active cortisol. Excess 11β-HSD1 or cortisol leads to insulin resistance and metabolic syndrome in animal models and in humans. Inhibiting 11β-HSD1 activity signifies a promising therapeutic strategy in the treatment of Type 2 diabetes and related diseases. Herein, the authors report two highly potent and selective small mol. inhibitors of human 11β-HSD1. While compound (I), a sulfonamide, functions as a simple substrate competitive inhibitor, compound (II), a triazole, shows the kinetic profile of a mixed inhibitor. Co-crystal structures reveal that both compounds occupy the 11β-HSD1 catalytic site, but present distinct mol. interactions with the protein. Strikingly, compound (II) interacts much closer to the cofactor NADP+ and likely modifies its binding. Together, the structural and kinetic analyses demonstrate two distinctive mol. inhibition mechanisms, providing valuable information for future inhibitor design.

Bioorganic & Medicinal Chemistry published new progress about Antidiabetic agents. 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Quality Control of 97009-67-1.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Wong, Ying-Chieh published the artcileLewis Basic Sulfide Catalyzed Electrophilic Bromocyclization of Cyclopropylmethyl Amide, Application In Synthesis of 97009-67-1, the main research area is electrophilic bromocyclization cyclopropylmethyl amide Lewis base sulfide catalyst; oxazoline oxazine stereoselective preparation.

A Lewis basic sulfide catalyzed electrophilic bromocyclization of cyclopropylmethyl amide has been developed. The catalytic protocol is applicable to both 1,1- and 1,2-substituted cyclopropylmethyl amides, giving oxazolines and oxazines, e.g. I and II, in good yields and excellent diastereoselectivity.

Organic Letters published new progress about Cyclization catalysts. 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Application In Synthesis of 97009-67-1.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Zhou, Mingwei published the artcileEfficient cyclopropanation of aryl/heteroaryl acetates and acetonitriles with vinyl diphenyl sulfonium triflate, Product Details of C10H8FN, the main research area is cyclopropanation aryl heteroaryl acetate acetonitrile; vinyl diphenyl sulfonium triflate cyclopropanation acetate acetonitrile.

A convenient method was developed for the cyclopropanation of aryl acetates and aryl acetonitrile using vinyl di-Ph sulfonium triflate salt. The newly developed conditions are simple, mild, and compatible with a wide range of functional groups, without the need to apply an inert atm., or alkali bases.

Tetrahedron Letters published new progress about Acetates Role: RCT (Reactant), RACT (Reactant or Reagent). 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Product Details of C10H8FN.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Kramm, Frederik published the artcileIron-Catalyzed Cycloisomerization and C-C Bond Activation to Access Non-canonical Tricyclic Cyclobutanes, COA of Formula: C10H8FN, the main research area is cyclopropyl enyne iron catalyst diastereoselective cycloisomerization; octahydrocyclobutacyclopenta pyrrole preparation; Cyclobutanes; Cycloisomerization; Cyclopropanes; Iron Catalysis; Rearrangement.

Cycloisomerizations are powerful skeletal rearrangements that allow the construction of complex mol. architectures in an atom-economic way. Here an unusual type of cyclopropyl enyne cycloisomerization that couples the process of a cycloisomerization with the activation of a C-C bond in cyclopropanes was presented . A set of substituted non-canonical tricyclic cyclobutanes were synthesized under mild conditions using [(Ph3P)2Fe(CO)(NO)]BF4 as catalyst in good to excellent yields with high levels of stereocontrol.

Angewandte Chemie, International Edition published new progress about Cyclobutanes Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, COA of Formula: C10H8FN.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Lee, Taegyo published the artcileRhodium-Catalyzed Enantioselective Silylation of Cyclopropyl C-H Bonds, Safety of 1-(4-Fluorophenyl)cyclopropanecarbonitrile, the main research area is rhodium catalyzed enantioselective silylation cyclopropylmethanol ethylsilane; chiral hydroxycyclopropanol preparation crystal structure; mol structure chiral hydroxycyclopropanol; carbon hydrogen bond activation silylation cyclopropylmethanol rhodium catalyst; kinetic isotope effect silylation cyclopropylmethanol rhodium catalyst; C−H activation; asymmetric catalysis; cyclopropanes; rhodium; silylation.

Hydrosilyl ethers, generated in situ by the dehydrogenative silylation of cyclopropylmethanols with diethylsilane, undergo asym., intramol. silylation of cyclopropyl C-H bonds in high yields and with high enantiomeric excesses in the presence of a Rh catalyst derived from a Rh precursor and the bisphosphine (S)-DTBM-SEGPHOS. The resulting enantioenriched oxasilolanes are suitable substrates for the Tamao-Fleming oxidation to form cyclopropanols with conservation of the ee value from the C-H silylation. Preliminary mechanistic data suggest that C-H cleavage probably is the turnover-limiting and enantioselectivity-determining step.

Angewandte Chemie, International Edition published new progress about C-H bond activation. 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Safety of 1-(4-Fluorophenyl)cyclopropanecarbonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Shuai, Bin published the artcileNickel-Catalyzed Favorskii-Type Rearrangement of Cyclobutanone Oxime Esters to Cyclopropanecarbonitriles, Quality Control of 97009-67-1, the main research area is cyclopropanecarbonitrile preparation; cyclobutanone oxime ester Favorskii rearrangement nickel catalyst.

A nickel-catalyzed base-promoted rearrangement of cyclobutanone oxime esters I (R1 = H, 4-tert-butyphenyl, 6-methoxynaphthalen-2-yl, phenylselanyl, etc.; R2 = H, Me, Ph; R3 = H, 2-naphthyl, 4-tert-butylphenyl, Ph, etc.; R2R3 = 1-adamantyl, 4-phenylcyclohexyl, cycloheptyl, etc.) to cyclopropanecarbonitriles II was developed. The ring opening of cyclobutanone oxime esters I occurs at the sterically less hindered side. A base-promoted nickelacyclobutane intermediate, formed in situ, is assumed to be involved in the formation of the product.

Synlett published new progress about Cyclopropanes Role: SPN (Synthetic Preparation), PREP (Preparation) (carbonitriles). 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Quality Control of 97009-67-1.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts