Chemokine receptor antagonists: overcoming developmental hurdles

R Horuk - Nature reviews Drug discovery, 2009 - nature.com
Chemokine receptors have a key role in the pathogenesis of autoimmune diseases,
inflammation and viral infection. However, with the exception of selective CCR5 antagonists …

[HTML][HTML] Lichenoid tissue reaction/interface dermatitis: clinical and histological perspectives

RD Sontheimer - Journal of investigative dermatology, 2009 - Elsevier
A number of uncommon, clinically diverse and poorly understood inflammatory skin
diseases are linked by the presence of a set of histopathological elements that have …

Visible Light Assisted Direct C3–H Arylation of Pyrido[1,2-a]pyrimidin-4-ones and Thiazolo[3,2-a]pyrimidin-5-ones

RT Bhawale, UA Kshirsagar - The Journal of Organic Chemistry, 2023 - ACS Publications
Metal-catalyst-free, organic dye-catalyzed C3–H arylation of pyrido [1, 2-a] pyrimidin-4-ones
using visible light irradiation was developed under mild reaction conditions. This …

Regioselective Direct C-3 Arylation of Imidazo[1,2-a]pyridines with Aryl Tosylates and Mesylates Promoted by Palladium–Phosphine Complexes

PY Choy, KC Luk, Y Wu, CM So, L Wang… - The Journal of Organic …, 2015 - ACS Publications
Direct C-3 arylation of imidazo [1, 2-a] pyridines with aryl tosylates and mesylates has been
accomplished by employing palladium (II) acetate associated with SPhos (2 …

Chemokine receptor antagonists: part 2

JE Pease, R Horuk - Expert opinion on therapeutic patents, 2009 - Taylor & Francis
Background: The first part of this two-part review discussed approaches to generating
antagonists for some of the CC chemokine receptors, including CCR1, CCR2, CCR3, and …

Metal free C-3 chalcogenation (sulfenylation and selenylation) of 4 H-pyrido [1, 2-a] pyrimidin-4-ones

P Ghosh, G Chhetri, S Das - RSC advances, 2021 - pubs.rsc.org
An expeditious metal free C-3 chalcogenation of 4H-pyrido [1, 2-a] pyrimidin-4-one has
been devised to synthesize diversely orchestrated 3-ArS/ArSe derivatives in high yields (up …

Small molecule CXCR3 antagonists

SP Andrews, RJ Cox - Journal of Medicinal Chemistry, 2016 - ACS Publications
Chemokines and their receptors are known to play important roles in disease. More than 40
chemokine ligands and 20 chemokine receptors have been identified, but, to date, only two …

Photoinduced Regioselective Chalcogenation and Thiocyanation of 4H‐Pyrido[1,2‐a] pyrimidin‐4‐ones Under Benign Conditions

AS Chillal, RT Bhawale… - European Journal of …, 2023 - Wiley Online Library
A lenient approach for regioselective C3− H chalcogenation and thiocyanation of 4H‐pyrido
[1, 2‐a] pyrimidin‐4‐ones is developed using visible light photocatalysis. This operationally …

Towards small‐molecule CXCR3 ligands with clinical potential

M Wijtmans, D Verzijl, R Leurs… - ChemMedChem …, 2008 - Wiley Online Library
The CXCR3 chemokine receptor was first discovered in 1996 and has been shown to play
an important role in several diseases, most of which are related to inflammation. This review …

Discovery, optimization, and in vivo evaluation of benzimidazole derivatives AM-8508 and AM-9635 as potent and selective PI3Kδ inhibitors

Y Shin, J Suchomel, M Cardozo… - Journal of Medicinal …, 2016 - ACS Publications
Lead optimization efforts resulted in the discovery of two potent, selective, and orally
bioavailable PI3Kδ inhibitors, 1 (AM-8508) and 2 (AM-9635), with good pharmacokinetic …