Synthesis and biological evaluation of analogs of AAL(S) for use as ceramide synthase 1 inhibitors. Issue 48 (4th November 2015)

• Record Type: Journal Article
• Authors: Toop, Hamish D.; Don, Anthony S.; Morris, Jonathan C.
• Is Part Of: Organic & biomolecular chemistry. Volume 13:Issue 48(2015)
• Page Start: 11593
• Page End: 11596
• Publication Date: 2015-11-04
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c5ob01931a
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : This work has led to the identification of a selective CerS1 inhibitor that is non-cytotoxic. Abstract : A convergent synthesis to access hydrophobic tail analogs and head group modifications of AAL(S) is described. The analogs synthesised were evaluated for their ability to inhibit ceramide synthase 1 and for their cytotoxicity in K562 cells. Our results have identified inhibitors which are non-cytotoxic yet maintain CerS1 inhibition.