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

doi:10.1016/j.ejmech.2014.01.027

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 journal › Article › peer-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 language	English
Pages (from-to)	184-194
Number of pages	11
Journal	European Journal of Medicinal Chemistry
Volume	75
DOIs	https://doi.org/10.1016/j.ejmech.2014.01.027
Publication status	Published - 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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/j.ejmech.2014.01.027

Cite this

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

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.",

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

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 ). ",

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doi = "10.1016/j.ejmech.2014.01.027",

language = "English",

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journal = "European Journal of Medicinal Chemistry",

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T2 - Structure-activity relationship focusing on the C17-side chain

AU - Kim, Kyeojin

AU - Maharjan, Sony

AU - Lim, Changjin

AU - Kim, Nam Jung

AU - Agrawal, Vijayendra

AU - Han, Young Taek

AU - Lee, Sujin

AU - An, Hongchan

AU - Yun, Hwayoung

AU - Choi, Hyun Jung

AU - Kwon, Young Guen

AU - Suh, Young Ger

N1 - 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 ).

PY - 2014/3/21

Y1 - 2014/3/21

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