scholarly journals Selective inhibition of p97 by chlorinated analogues of dehydrocurvularin

2016 ◽  
Vol 14 (25) ◽  
pp. 5918-5921 ◽  
Author(s):  
Joseph Tillotson ◽  
Bharat P. Bashyal ◽  
MinJin Kang ◽  
Taoda Shi ◽  
Fabian De La Cruz ◽  
...  
Keyword(s):  
Aromatic Ring ◽  
Selective Inhibition ◽  
Chlorine Atoms ◽  
Covalent Inhibition

Through the addition of chlorine atoms to the aromatic ring of 10(11)-dehydrocurvularin, covalent inhibition was tuned for p97 selectivity relative to the proteasome.

Dependence of the conversion of chlorophenols by rhodococci on the number and position of chlorine atoms in the aromatic ring

Microbiology ◽  
2000 ◽  
Vol 69 (1) ◽  
pp. 40-47 ◽  
Author(s):  
Z. I. Finkel’shtein ◽  
B. P. Baskunov ◽  
E. L. Golovlev ◽  
O. V. Moiseeva ◽  
J. Vervoort ◽  
...  
Keyword(s):  
Aromatic Ring ◽  
Chlorine Atoms

13C and 119Sn NMR evidence of the presence and extent of σ-π conjugation in some benzyltin compounds and their complexes

1988 ◽  
Vol 53 (3) ◽  
pp. 571-580 ◽  
Author(s):  
Jaroslav Holeček ◽  
Antonín Lyčka ◽  
Karel Handlíř ◽  
Milan Nádvorník
Keyword(s):  
Nmr Spectroscopy ◽  
Coordination Number ◽  
Aromatic Ring ◽  
Electronic System ◽  
Methyl Groups ◽  
Chlorine Atoms ◽  
Nmr Data ◽  
Relative Extent ◽  
119Sn Nmr

The 13C and 119Sn NMR spectroscopy has been used to study the compounds types (C6H5CH2)4-nSn(CH3)n and (C6H5CH2)4-nSnCln (n = 0 - 3) in media of non-coordinating (deuteriochloroform) and coordinating (hexadeuteriomethyl sulphoxide) solvents. The analysis of the NMR data has confirmed the presence and established the relative extent of participation of the σ-π conjugative connection of the polarized σ(Sn-C) bond with the adjacent π electronic system of the aromatic ring in the Sn-CH2-C6H5 grouping. The extent of σ-π conjugation decreases with decreasing number of methyl groups in the compounds (C6H5CH2)4-nSn(CH3)n and with increasing number of chlorine atoms in the compounds (C6H5CH2)4-nSnCln and with increasing coordination number of the central tin atom in the complexes of the compounds (C6H5CH2)4-nSnCln.x(C2H3)2SO.

scholarly journals Transformation of 2H-1,2,3-benzothiadiazine 1,1-dioxides variously substituted at the aromatic ring, via nucleophilic substitution and demethylation reactions

2020 ◽  
Author(s):  
Imre Gyűjtő ◽  
Márta Porcs-Makkay ◽  
Ernák Ferenc Várda ◽  
Gyöngyvér Pusztai ◽  
Gábor Tóth ◽  
...  
Keyword(s):  
Nucleophilic Substitution ◽  
Functional Groups ◽  
Aromatic Ring ◽  
Methoxy Group ◽  
Medicinal Chemistry ◽  
Building Blocks ◽  
Chlorine Atoms ◽  
New Methods ◽  
Pharmacological Interest

2H‑1,2,3‑Benzothiadiazine 1,1-dioxides are a class of compounds of pharmacological interest. After earlier studies carried out at our laboratory on various transformations (alkylation, acylation, reduction) at the hetero ring, the present manuscript focuses on the transformation of substituents at the aromatic carbocycle, including nucleophilic substitution of chlorine atoms and demethylation of the methoxy group with amines. The new methods described here allow the introduction of versatile functional groups on the aromatic ring, making these compounds useful building blocks for organic and medicinal chemistry applications.

Stroma-derived factor 1alpha induces a selective inhibition of human erythroid development via the functional upregulation of Fas/CD95 ligand

2000 ◽  
Vol 111 (2) ◽  
pp. 432-440 ◽  
Author(s):  
Davide Gibellini ◽  
Alessandra Bassini ◽  
Maria Carla Re ◽  
Cristina Ponti ◽  
Sebastiano Miscia ◽  
...  
Keyword(s):  
Selective Inhibition ◽  
Cd95 Ligand ◽  
Erythroid Development

Increased response preparation overshadows neurophysiological evidence of proactive selective inhibition.

2018 ◽  
Vol 11 (1) ◽  
pp. 1-17 ◽  
Author(s):  
Neil M. Drummond ◽  
Erin K. Cressman ◽  
Anthony N. Carlsen
Keyword(s):  
Selective Inhibition ◽  
Response Preparation

Selective inhibition of chemokine CCL2/MCP-1 reduces experimental pulmonary hypertension

Pneumologie ◽  
2013 ◽  
Vol 67 (05) ◽  
Author(s):  
D Kosanovic ◽  
BK Dahal ◽  
C Vroom ◽  
E Bieniek ◽  
H Ardeschir Ghofrani ◽  
...  
Keyword(s):  
Pulmonary Hypertension ◽  
Selective Inhibition

Selective Inhibition of Thromboxane Synthetase with Dazoxiben - Basis of Its Inhibitory Effect on Platelet Adhesion

1983 ◽  
Vol 49 (02) ◽  
pp. 096-101 ◽  
Author(s):  
V C Menys ◽  
J A Davies
Keyword(s):  
Arachidonic Acid ◽  
Platelet Adhesion ◽  
Fold Increase ◽  
Selective Inhibition ◽  
Inhibitory Effect ◽  
Selective Inhibitor ◽  
Coated Glass ◽  
Thromboxane Synthetase ◽  
Pre Treatment

SummaryPlatelet adhesion to rabbit aortic subendothelium or collagen-coated glass was quantitated in a rotating probe device by uptake of radio-labelled platelets. Under conditions in which aspirin had no effect, dazoxiben, a selective inhibitor of thromboxane synthetase, reduced platelet adhesion to aortic subendothelium by about 40% but did not affect adhesion to collagen-coated glass. Pre-treatment of aortic segments with 15-HPETE, a selective inhibitor of PGI2-synthetase, abolished the inhibitory effect of dazoxiben on adhesion. Concentrations of 6-oxo-PGFlα in the perfusate were raised in the presence of dazoxiben alone, and following addition of thrombin (10 units/ml) there was a 2-3 fold increase in concentration. Perfusion of damaged aorta with platelets labelled with (14C)-arachidonic acid in the presence of thrombin and dazoxiben resulted in the appearance of (14C)-labelled-6-oxo-PGFiα. Inhibition of thromboxane synthetase limits platelet adhesion probably by promoting vascular synthesis of PGI2 from endoperoxides liberated from adherent platelets, which subsequently promotes detachment of cells from the surface.

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