Search Results

You searched for all publications:

with publication states 'Published (Approved)'

Search Again...

Author Name

Author Affiliation

Author ORCID

Title of Publication

DOI

Data DOI

Type of Publication (check all that apply) select all

Book Chapter

Conference Paper

Editors' Note

Journal Paper

Magazine Article

Poster

Report

Thesis

Title of Journal

Title of Conference

Peer Reviewed:

Yes No Either

Title of Magazine

Abstract

Keywords

Tags

Funding

Diamond Proposal Number

ISBN

BookChapter

Open Access:

Yes No Either

Published In or After Help

Published In or Before Help

These results only include publications that have been reviewed and processed by Diamond Light Source. To also view papers that have not yet been processed click here.

You can use the folder icon under Actions to collate papers as required. You can then click on View Folder in the left-hand navigation to review and/or download your folder.

Exact matches
Related results

One item found (0 items not approved).1

Instruments / Technical Area	Publication Details	Published	Actions
I04-1-Macromolecular Crystallography (fixed wavelength)	[b]-Annulated halogen-substituted indoles as potential DYRK1A inhibitors Christian Lechner , Maren Flaßhoff , Hannes Falke , Lutz Preu , Nadége Loaëc , Laurent Meijer , Stefan Knapp , Apirat Chaikuad , Conrad Kunick Molecules 24 DOI: 10.3390/molecules24224090 Diamond Proposal Number(s): [8421] Open Access Show Abstract ▼ Abstract: Since hyperactivity of the protein kinase DYRK1A is linked to several neurodegenerative disorders, DYRK1A inhibitors have been suggested as potential therapeutics for Down syndrome and Alzheimer’s disease. Most published inhibitors to date suffer from low selectivity against related kinases or from unfavorable physicochemical properties. In order to identify DYRK1A inhibitors with improved properties, a series of new chemicals based on [b]-annulated halogenated indoles were designed, synthesized, and evaluated for biological activity. Analysis of crystal structures revealed a typical type-I binding mode of the new inhibitor 4-chlorocyclohepta[b]indol-10(5H)-one in DYRK1A, exploiting mainly shape complementarity for tight binding. Conversion of the DYRK1A inhibitor 8-chloro-1,2,3,9-tetrahydro-4H-carbazol-4-one into a corresponding Mannich base hydrochloride improved the aqueous solubility but abrogated kinase inhibitory activity.	Nov 2019

Publications Database

Search Results

You searched for all publications:

Search Again...

Subject Areas (check all that apply) select all

Instruments used to collect data (check all that apply) select all

Collaborations involved (check all that apply) select all

Diamond Offline Facilities used

Relevant Technical Areas (check all that apply) select all

Menu for Anonymous User