Exploration of α-aminophosphonate N-derivatives as novel, potent and selective inhibitors of protein tyrosine phosphatases

Q Wang, M Zhu, R Zhu, L Lu, C Yuan, S Xing…

Index: Wang, Qingming; Zhu, Miaoli; Zhu, Ruiting; Lu, Liping; Yuan, Caixia; Xing, Shu; Fu, Xueqi; Mei, Yuhua; Hang, Qingwei European Journal of Medicinal Chemistry, 2012 , vol. 49, p. 354 - 364

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Citation Number: 34

Abstract

Seventeen α-aminophosphonates are synthesized. Their compositions and structures are established by EA, UV, FT-IR, 1H NMR, 13C NMR, 31P NMR and ESI-MS. Compounds 1–4 are confirmed by X-ray crystallography. PTP inhibition shows compounds 1–5, 12, 15 are moderate competitive inhibitors with some selectivity. The most potent inhibitor is compound 5 with the lowest IC50 value about 6.64 μM against PTP1B, about 2-fold and 25-fold ...