Title of article :
Design, synthesis, and discovery of stilbene derivatives based on lithospermic acid B as potent protein tyrosine phosphatase 1B inhibitors
Author/Authors :
Mankil Jung، نويسنده , , Yongnam Lee، نويسنده , , Moonsoo Park، نويسنده , , Hanjo Kim، نويسنده , , Heekyeong Kim، نويسنده , , Eunyoung Lim، نويسنده , , Jungae Tak، نويسنده , , Minjoo Sim، نويسنده , , Dongeun Lee، نويسنده , , Namsoo Park، نويسنده , , Won Keun Oh، نويسنده , , Kyu Yeon Hur، نويسنده , , Eun Seok Kang، نويسنده , , Hyun-Chul Lee ، نويسنده ,
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.
