School of Chemical Sciences, The University of Auckland, 23 Symonds St, Auckland, 1010, New Zealand; The Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland, 1010, New Zealand.
The Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland, 1010, New Zealand; Auckland Cancer Society Research Centre, School of Medical Sciences, The University of Auckland, Private Bag 92019, Auckland, 1010, New Zealand.
Eur J Med Chem. 2019 Sep 1;177:235-246. doi: 10.1016/j.ejmech.2019.05.052. Epub 2019 May 23.
Culicinin D is a 10 amino acid peptaibol containing a rare and synthetically challenging (2S,4S,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.
Culicinin D 是一种 10 个氨基酸组成的肽类化合物，含有一个罕见且具有挑战性的（2S,4S,6R）-AHMOD 残基，对 MDA-MB-468 细胞表现出强烈的抗增殖活性。我们进行了一项 SAR 研究，重点研究了 AHMOD 残基的取代，最终揭示了 6-羟基或 6-酮取代基对于保持强效的低纳摩尔抗增殖活性是必不可少的。
