Discovery of a potent, orally available furopyridine derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor

S Hagihara, K Ishizawa, M Kikuchi, Y Kawano… - Bioorganic & Medicinal …, 2024 - Elsevier
… effects, similar to BET inhibitors. This study identified furopyridine derivatives 7 and 8 with
high … induced by CD28 co-stimulation leads to the discovery of a first bromodomain inhibitor

BET inhibitors as anticancer agents: A patent review

I Ali, G Choi, K Lee - Recent Patents on Anti-Cancer Drug …, 2017 - ingentaconnect.com
… Several BET bromodomain inhibitors are currently under clinical devel… inhibitors is based
on the furopyridine compounds reported by GSK (Fig. 33). Majority of these furopyridines have …

Small molecule inhibitors of bromodomain–acetyl-lysine interactions

M Brand, AM Measures, BG Wilson… - ACS chemical …, 2015 - ACS Publications
… design of dual kinase–bromodomain inhibitors that possess complementary pharmacology
… (47, 48) Additionally, researchers at GSK reported the novel thienopyridinone, furopyridine

Successes and challenges in the development of BD1-selective BET inhibitors: a patent review

M Viviano, A Cipriano, E Fabbrizi, A Feoli… - Expert Opinion on …, 2024 - Taylor & Francis
… Pomeratnz et al. described a series of dual kinase-bromodomain inhibitors with preferential
binding … Fused 1,4-diazepines as BET bromodomain inhibitors and their preparation patent …

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

EJ Faivre, KF McDaniel, DH Albert, SR Mantena… - Nature, 2020 - nature.com
… through their bromodomains to regulate gene transcription. Dual-bromodomain BET inhibitors
(DbBi) that bind with similar affinities to the first (BD1) and second (BD2) bromodomains of …

[PDF][PDF] Bromodomain as New Targets in Drug Discovery

ACB Melchior, AR Pavan… - Biochem …, 2015 - pdfs.semanticscholar.org
inhibitors have been reported in the literature. Researchers have described thienopyridinone,
furopyridine and … In summary, this editorial highlights the use of bromodomain inhibitors as …

… of a potent orally available pyrazolopyridone derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor

S Hagihara, K Ishizawa, K Soga, T Honjo… - Bioorganic & Medicinal …, 2024 - Elsevier
… Clinical studies have shown that inhibitors of bromodomain and extra-terminal domain (BET…
bioavailable BD1-selective inhibitors. In this study, we obtained a BD1 inhibitor, a more …

Copper‐Catalyzed Tandem Imine Formation, Sonogashira Coupling and Intramolecular Hydroamination: A Facile Synthesis of 3‐Aryl‐γ− carbolines

S Dhiman, S Rhodes, D Kumar, A Kumar… - …, 2017 - Wiley Online Library
… γ-carboline derivatives act as BET bromodomain inhibitor.12 Because of their importance
in … one-pot synthesis of isoquinolines, furopyridines, and thienopyridiens using Pd-catalyzed …

The Groebke‐Blackburn‐Bienaymé Reaction

A Boltjes, A Dömling - European Journal of Organic Chemistry, 2019 - Wiley Online Library
Imidazo[1,2‐a]pyridine is a well‐known scaffold in many marketed drugs, such as Zolpidem,
Minodronic acid, Miroprofen and DS‐1 and it also serves as a broadly applied …

Development of an intracellular quantitative assay to measure compound binding kinetics

CS Lay, DA Thomas, JP Evans, M Campbell… - Cell chemical …, 2022 - cell.com
… Here, we describe an intracellular NanoBRET competition assay that can be used to quantify
cellular kinetic rates of compound binding to nanoluciferase-fused bromodomain and extra-…