Glucal-conjugated sterols as novel vascular leakage blocker: Structure-activity relationship focusing on the C17-side chain

Kyeojin Kim, Sony Maharjan, Changjin Lim, Nam Jung Kim, Vijayendra Agrawal, Young Taek Han, Sujin Lee, Hongchan An, Hwayoung Yun, Hyun Jung Choi, Young Guen Kwon, Young Ger Suh

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

A series of glucal-conjugated sterols as novel vascular leakage blocker were identified through design, synthesis and biologically evaluation. In addition, the structure-activity relationship (SAR) of the glucal-conjugated sterols focusing on the C17-side chain was also established. The sterol analogs linked with the rigid C17-side chain side chains exhibited potent cell survival activities. In particular, analog 21l, which possesses a cyclopentyl oxime moiety, was shown to have excellent pharmacological effects on retinal vascular leakage in a diabetic mouse model.

Original languageEnglish
Pages (from-to)184-194
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume75
DOIs
Publication statusPublished - 2014 Mar 21

Bibliographical note

Funding Information:
This work is supported by a grant from the Bio & Medical Technology Development Program of the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (MEST) ( NRF-2011-0019267 ) and by the National Research Foundation of Korea (NRF) grant for the Global Core Research Center (GCRC) funded by the Korea Government (MSIP) (No. 2011-0030001 ).

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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