4.7 Article

Discovery, Synthesis, and In Vitro Characterization of 2,3 Derivatives of 4,5,6,7-Tetrahydro-Benzothiophene as Potent Modulators of Retinoic Acid Receptor-Related Orphan Receptor γt

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Chemistry, Medicinal

Discovery of 2H-chromone-4-one based sulfonamide derivatives as potent retinoic acid receptor-related orphan receptor γt inverse agonists

Lei Chen et al.

Summary: A novel ROR γt inverse agonist, compound c9, was discovered and demonstrated its potential in treating autoimmune diseases through in vivo experiments.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Multidisciplinary Sciences

Discovery of a novel RORγ antagonist with skin-restricted exposure for topical treatment of mild to moderate psoriasis

Suxing Liu et al.

Summary: A novel topical drug was discovered with desired properties for the treatment of moderate to severe psoriasis, showing high exposure in skin but low in plasma, which suppressed IL-17 gene transcription and reduced IL-17 cytokine secretion. This new option demonstrated efficacy in psoriasis-like skin inflammation models, indicating it may be a suitable treatment for inflammatory disorders accessible locally.

SCIENTIFIC REPORTS (2021)

Article Chemistry, Medicinal

Discovery of [1,2,4]Triazolo[1,5-a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists

Ryota Nakajima et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

Article Chemistry, Medicinal

Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt

Christian Gege et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

Review Biochemistry & Molecular Biology

RORγ Structural Plasticity and Druggability

Mian Huang et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

Article Chemistry, Medicinal

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yI)sulfones as Selective, Orally Active RORγt Inverse Agonists

James J. -W. Duan et al.

ACS MEDICINAL CHEMISTRY LETTERS (2019)

Article Chemistry, Medicinal

Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists

Jerome Amaudrut et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2019)

Article Chemistry, Medicinal

Discovery of N-indanyl benzamides as potent RORγt inverse agonists

Jinlong Tian et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Chemistry, Multidisciplinary

Molecular dynamics simulations on RORγt: insights into its functional agonism and inverse agonism

Cong-min Yuan et al.

ACTA PHARMACOLOGICA SINICA (2019)

Article Biochemistry & Molecular Biology

5,6,7,8-Tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivatives as inhibitors of full-length RORγt

Chuyu Lao et al.

BIOORGANIC CHEMISTRY (2019)

Article Biochemistry & Molecular Biology

Identification of novel quinazolinedione derivatives as RORγt inverse agonist

Yoshiyuki Fukase et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds

Junya Shirai et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2018)

Article Chemistry, Medicinal

Sulfoximines as potent RORc inverse agonists

Gilles Ouvry et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2018)

Article Chemistry, Medicinal

Discovery of carbazole carboxamides as novel RORγt inverse agonists

Yafei Huang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Medicinal

Potent and Orally Bioavailable Inverse Agonists of RORγt Resulting from Structure-Based Design

Frank Narjes et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Medicinal

N-Arylsulfonyl Indolines as Retinoic Acid Receptor-Related Orphan Receptor γ (RORγ) Agonists

Christelle Doebelin et al.

CHEMMEDCHEM (2016)

Article Medicine, General & Internal

The Nuclear Receptor, RORγ, Regulates Pathways Necessary for Breast Cancer Metastasis

Tae Gyu Oh et al.

EBIOMEDICINE (2016)

Article Multidisciplinary Sciences

Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin

Susan H. Smith et al.

PLOS ONE (2016)

Article Chemistry, Medicinal

Discovery of novel pyrazole-containing benzamides as potent ROR gamma inverse agonists

Tao Wang et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2015)

Article Chemistry, Medicinal

Discovery of biaryl carboxylamides as potent RORγ inverse agonists

Jianhua Chao et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2015)

Article Chemistry, Medicinal

Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists

Benjamin P. Fauber et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2015)

Article Chemistry, Medicinal

Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors

Yonghui Wang et al.

ACS MEDICINAL CHEMISTRY LETTERS (2015)

Article Multidisciplinary Sciences

Identification of an allosteric binding site for RORγt inhibition

Marcel Scheepstra et al.

NATURE COMMUNICATIONS (2015)

Article Biochemistry & Molecular Biology

Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl) amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors

Yonghui Wang et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2014)

Article Chemistry, Medicinal

A reversed sulfonamide series of selective RORc inverse agonists

Monique B. van Niel et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2014)

Article Chemistry, Medicinal

iLOGP: A Simple, Robust, and Efficient Description of n-Octanol/Water Partition Coefficient for Drug Design Using the GB/SA Approach

Antoine Daina et al.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2014)

Article Multidisciplinary Sciences

Oxysterols are agonist ligands of RORγt and drive Th17 cell differentiation

Pejman Soroosh et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2014)

Article Chemistry, Medicinal

Discovery of Tertiary Amine and Indole Derivatives as Potent RORγt Inverse Agonists

Ting Yang et al.

ACS MEDICINAL CHEMISTRY LETTERS (2014)

Article Chemistry, Medicinal

Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc

Benjamin P. Fauber et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2013)

Letter Cell Biology

RORtIL-17 neutrophils play a critical role in hepatic ischemiareperfusion injury

Zhongming Tan et al.

JOURNAL OF MOLECULAR CELL BIOLOGY (2013)

Article Chemistry, Medicinal

Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors

Jun R. Huh et al.

ACS MEDICINAL CHEMISTRY LETTERS (2013)

Article Biochemical Research Methods

Analysis of protein-ligand interactions by fluorescence polarization

Ana M. Rossi et al.

NATURE PROTOCOLS (2011)

Article Biochemistry & Molecular Biology

A second class of nuclear receptors for oxysterols: Regulation of RORα and RORγ activity by 24S-hydroxycholesterol (cerebrosterol)

Yongjun Wang et al.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS (2010)

Article Chemistry, Multidisciplinary

ESOL: Estimating aqueous solubility directly from molecular structure

JS Delaney

JOURNAL OF CHEMICAL INFORMATION AND COMPUTER SCIENCES (2004)