Details

Autor(en) / Beteiligte

• Toop, Hamish D
• Don, Anthony S
• Morris, Jonathan C

Titel

Synthesis and biological evaluation of analogs of AAL(S) for use as ceramide synthase 1 inhibitorsElectronic supplementary information (ESI) available: Synthetic procedures and characterisation data for all new compounds. See DOI: 10.1039/c5ob01931a

Erscheinungsjahr

2015-12

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• 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. This work has led to the identification of a selective CerS1 inhibitor that is non-cytotoxic.