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 journalArticle

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

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Calcium Gluconate
Sterols
Structure-Activity Relationship
Blood Vessels
Retinal Vessels
Oximes
Cell Survival
Cells
Pharmacology

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this

Kim, Kyeojin ; Maharjan, Sony ; Lim, Changjin ; Kim, Nam Jung ; Agrawal, Vijayendra ; Han, Young Taek ; Lee, Sujin ; An, Hongchan ; Yun, Hwayoung ; Choi, Hyun Jung ; Kwon, Young Guen ; Suh, Young Ger. / Glucal-conjugated sterols as novel vascular leakage blocker : Structure-activity relationship focusing on the C17-side chain. In: European Journal of Medicinal Chemistry. 2014 ; Vol. 75. pp. 184-194.
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Glucal-conjugated sterols as novel vascular leakage blocker : Structure-activity relationship focusing on the C17-side chain. / Kim, Kyeojin; Maharjan, Sony; Lim, Changjin; Kim, Nam Jung; Agrawal, Vijayendra; Han, Young Taek; Lee, Sujin; An, Hongchan; Yun, Hwayoung; Choi, Hyun Jung; Kwon, Young Guen; Suh, Young Ger.

In: European Journal of Medicinal Chemistry, Vol. 75, 21.03.2014, p. 184-194.

Research output: Contribution to journalArticle

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