Výsledky vyhledávání - "Sylwia Stachura"

Discovery of 2,6-difluorobenzyl ether series of phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists

Autor: Bin Jiang, Sylwia Stachura, T. G. Murali Dhar, Carolyn A. Weigelt, Dauh Rurng Wu, Jingwu Duan, Luisa M. Salter–Cid, Javed Khan, Ding Ren Shen, Melissa Yarde, Qihong Zhao, Zhonghui Lu, Percy H. Carter, John S. Sack, Max Ruzanov

Publikováno v: Bioorganicmedicinal chemistry letters. 30(19)

In an effort to discover oral inverse agonists of RORγt to treat inflammatory diseases, a new 2,6–difluorobenzyl ether series of cyclopentyl sulfones were found to be surprisingly more potent than the corresponding alcohol derivatives. When combin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79d78507decbe1c2b5ea2335c53b8ab6
https://pubmed.ncbi.nlm.nih.gov/32736080

Zobrazit plný text záznamu

Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists

Publikováno v: Bioorganicmedicinal chemistry letters. 30(12)

Substituted benzyloxy aryl compound 2 was identified as an RORγt agonist. Structure based drug design efforts resulted in a potent and selective tricyclic compound 19 which, when administered orally in an MC38 mouse tumor model, demonstrated a desir

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d28391368dbe9fe0275182d85ed69ba6
https://pubmed.ncbi.nlm.nih.gov/32334911

Zobrazit plný text záznamu

Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 35:127778

The discovery of a series of substituted diarylether compounds as retinoic acid related orphan receptor γt (RORγt) agonists is described. Compound 1 was identified from deck mining as a RORγt agonist. Hit-to-lead optimization led to the identifica

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6bcbeb08e68c5a36002135e73f0931e
https://doi.org/10.1016/j.bmcl.2021.127778

Zobrazit plný text záznamu

Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors

Autor: Carolyn A. Weigelt, Xiaomei Gu, Lan-Ying Qin, Christine B. Goldstine, Sylwia Stachura, Jenny Xie, Zheming Ruan, T. G. Murali Dhar, Donna L. Pedicord, Michael A. Poss, Luisa Salter-Cid, Rajeev S. Bhide, Percy H. Carter, James Neels, John S. Sack, Stefan Ruepp, Kevin Stefanski, Paul Davies, Stacey Skala

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 26:4256-4260

Aberrant Class I PI3K signaling is a key factor contributing to many immunological disorders and cancers. We have identified 4-amino pyrrolotriazine as a novel chemotype that selectively inhibits PI3Kδ signaling despite not binding to the specificit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cdaa3a62c46009198cffe25f36688ef7
https://doi.org/10.1016/j.bmcl.2016.07.047

Zobrazit plný text záznamu

Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists

Autor: Javed Khan, Dhanya Kumar Raut, Sylwia Stachura, Qihong Zhao, Jingwu Duan, Melissa Yarde, Bin Jiang, Hemalatha Hemagiri, Arvind Mathur, Ananta Karmakar, Michael Galella, T. G. Murali Dhar, John S. Sack, Percy H. Carter, Luisa Salter-Cid, Arun Kumar Gupta, Carolyn A. Weigelt, Dauh-Rurng Wu, Ding-Ren Shen

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 30:127392

A novel series of cis-3,4-diphenylpyrrolidines were designed as RORγt inverse agonists based on the binding conformation of previously reported bicyclic sulfonamide 1. Preliminary synthesis and structure–activity relationship (SAR) study establish

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7bcbc80bdfe799857c1dc059bd62be3
https://doi.org/10.1016/j.bmcl.2020.127392

Zobrazit plný text záznamu

Triazolopyrimidines identified as reversible myeloperoxidase inhibitors

Publikováno v: MedChemComm. 8(11)

Myeloperoxidase, a mammalian peroxidase involved in the immune system as an anti-microbial first responder, can produce hypochlorous acid in response to invading pathogens. Myeloperoxidase has been implicated in several chronic pathological diseases

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6938309a24e135aae00aaf681ec2a84d
https://pubmed.ncbi.nlm.nih.gov/30108726

Zobrazit plný text záznamu

Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors

Publikováno v: Bioorganicmedicinal chemistry letters. 27(14)

A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of the pyrrolopyridazine core with aryl groups provided exceptional biochemical potency against JAK1 and JAK3 wh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::253daa677cbcba359ab77a6e70a14d27
https://pubmed.ncbi.nlm.nih.gov/28539220

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání