Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377397 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
Abstract
Dihydroxy stilbene derivatives were designed based on lithospermic acid B and were prepared from 4-(chloromethyl)benzoic acid. The inhibitory activities of the novel compounds against protein tyrosine phosphatase 1B (PTP1B) were evaluated. 3,4-Dihydroxy stilbene carbonyl compounds (7, 11b, 27b) inhibited PTP1B with IC50 values comparable to molybdate, while the conjugation-extended compound (15b) showed inhibition 3-fold better than preclinical RK682. The introduction of electron withdrawing groups or amides into the second phenyl ring, or extension of the conjugation into the stilbene molecule may increase stability of the generated radicals.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Mankil Jung, Yongnam Lee, Moonsoo Park, Hanjo Kim, Heekyeong Kim, Eunyoung Lim, Jungae Tak, Minjoo Sim, Dongeun Lee, Namsoo Park, Won Keun Oh, Kyu Yeon Hur, Eun Seok Kang, Hyun-Chul Lee,