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PF‐8380 and Closely Related Analogs: Synthesis and Structure–Activity Relationship towards Autotaxin Inhibition and Glioma Cell Viability
Author(s) -
StCœur PatrickDenis,
Ferguson Dean,
Morin Pier Jr,
Touaibia Mohamed
Publication year - 2013
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201200395
Subject(s) - autotaxin , chemistry , temozolomide , moiety , stereochemistry , cell culture , isoflavonoid , viability assay , glioma , biochemistry , cell , cancer research , biology , flavonoid , receptor , genetics , lysophosphatidic acid , antioxidant
A series of PF‐8380 analogs, a recently developed autotaxin inhibitor, was explored. Inhibition of autotaxin by these analogs, as well as by all PF‐8380 synthetic intermediates, shows the importance of meta ‐dichlorobenzyl and benzo[ d ]oxazol‐2(3 H )‐one fragments. However, analogs 8 and 9 , bearing only the benzo[ d ]oxazol‐2(3 H )‐one moiety, are more cytotoxic on the LN229 glioblastoma cell line than PF‐8380 and temozolomide (TMZ).