Journal
ARCHIV DER PHARMAZIE
Volume 346, Issue 2, Pages 91-97Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201200395
Keywords
Autotaxin; Glioma cell; Inhibitory activity; Synthesis; Structur-activity relationship
Funding
- Brain Tumour Foundation of Canada
- Beatrice Hunter Cancer Research Institute
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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).
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