Synthesis and antiproliferative activity of culicinin D analogues containing simplified AHMOD-based residues

Culicinin D is a 10 amino acid peptaibol containing a rare and synthetically challenging (2S,45,6R)-AHMOD residue, that exhibits potent antiproliferative activity against MDA-MB-468 cells. An SAR study focusing on replacement of the AHMOD residue was undertaken, culminating in the revelation that a 6-hydroxy or 6-keto substituent was essential to retain potent low nanomolar antiproliferative activity. (C) 2019 Elsevier Masson SAS. All rights reserved.