Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594108 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
A series of optical amino acid diosgenyl esters and diosgenyl salicylate conjugates were designed and synthesized to develop new anticancer and anti-inflammatory agents. The analogue 9c that contains an 6-aminohexanoic acid residue at C-3 of diosgenin exhibits higher potency against all three tumor cell lines with IC50 values ranging from 4.7 μM in C26 cells to 14.6 μM in Hep G2 cells. In addition, seven of newly synthesized compounds significantly inhibit xylene-induced ear edema and exhibit comparable or better anti-inflammatory activities than those of diosgenin and aspirin. Furthermore, preliminary structure-activity relationship studies demonstrate that diosgenyl salicylate conjugates have stronger anti-inflammatory activities than amino acid diosgenyl esters.
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Authors
Baozhan Huang, Dan Du, Rui Zhang, Xiaohua Wu, Zhihua Xing, Yang He, Wen Huang,