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PF-8380 and Closely Related Analogs: Synthesis and Structure-Activity Relationship Towards Autotaxin Inhibition and Glioma Cell Viability

Patrick-Denis St-Cœur, Dean Ferguson, Pier Morin Jr, Mohamed Touaibia

Arch Pharm (Weinheim). 2013 Feb;346(2):91-7.

PMID: 23300119

Abstract:

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(3H)-one fragments. However, analogs 8 and 9, bearing only the benzo[d]oxazol-2(3H)-one moiety, are more cytotoxic on the LN229 glioblastoma cell line than PF-8380 and temozolomide (TMZ).

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1144035539 PF-8380 PF-8380 1144035-53-9 Price
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