Ontology highlight
ABSTRACT:
SUBMITTER: Bai A
PROVIDER: S-EPMC4443482 | biostudies-literature | 2014 Dec
REPOSITORIES: biostudies-literature
Bai Aiping A Szulc Zdzislaw M ZM Bielawski Jacek J Pierce Jason S JS Rembiesa Barbara B Terzieva Silva S Mao Cungui C Xu Ruijuan R Wu Bill B Clarke Christopher J CJ Newcomb Benjamin B Liu Xiang X Norris James J Hannun Yusuf A YA Bielawska Alicja A
Bioorganic & medicinal chemistry 20141022 24
Acid ceramidase (ACDase) is being recognized as a therapeutic target for cancer. B13 represents a moderate inhibitor of ACDase. The present study concentrates on the lysosomal targeting of B13 via its N,N-dimethylglycine (DMG) esters (DMG-B13 prodrugs). Novel analogs, the isomeric mono-DMG-B13, LCL522 (3-O-DMG-B13·HCl) and LCL596 (1-O-DMG-B13·HCl) and di-DMG-B13, LCL521 (1,3-O, O-DMG-B13·2HCl) conjugates, were designed and synthesized through N,N-dimethyl glycine (DMG) esterification of the hydr ...[more]