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Discovery and structure-activity relationships of spiroindolines as novel inducers of oligodendrocyte progenitor cell differentiation.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2020 Mar 15; Vol. 28 (6), pp. 115348. Date of Electronic Publication: 2020 Jan 28. - Publication Year :
- 2020
-
Abstract
- A novel series of spiroindoline derivatives was discovered for use as inducers of oligodendrocyte progenitor cell (OPC) differentiation, resulting from optimization of screening hit 1. Exploration of structure-activity relationships led to compound 18, which showed improved potency (rOPC EC <subscript>50</subscript>  = 0.0032 μM). Furthermore, oral administration of compound 18 significantly decreased clinical severity in an experimental autoimmune encephalomyelitis (EAE) model.<br />Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2020 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Cell Differentiation drug effects
Dose-Response Relationship, Drug
Encephalomyelitis, Autoimmune, Experimental pathology
Female
Indoles chemical synthesis
Indoles chemistry
Mice
Mice, Inbred C57BL
Molecular Structure
Rats
Rats, Wistar
Spiro Compounds chemical synthesis
Spiro Compounds chemistry
Structure-Activity Relationship
Drug Discovery
Encephalomyelitis, Autoimmune, Experimental drug therapy
Indoles pharmacology
Oligodendrocyte Precursor Cells drug effects
Spiro Compounds pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 28
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 32046916
- Full Text :
- https://doi.org/10.1016/j.bmc.2020.115348