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.
Bibliographical noteFunding 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
- Drug Discovery
- Organic Chemistry