3 years ago

Benzo[c][1,2,5]thiadiazole Derivatives : A New Class of Potent Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (SHP2) Inhibitors

Benzo[c][1,2,5]thiadiazole Derivatives : A New Class of Potent Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (SHP2) Inhibitors
The Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) is an oncogenic phosphatase linked to various kinds of cancers. Consequently, SHP2 has emerged as a promising target for novel anti-cancer agents. Using scaffold-hopping strategy, a series of benzo[c][1,2,5]thiadiazole derivatives was designed from PTP1B inhibitors with 1H-2,3-Dihydroperimidine motif, synthesized and evaluated their biological activities against PTP1B and SHP2. Among them, the representative compound 11g displayed SHP2 inhibitory activity with IC50 of 2.11±0.99 μM, exhibited 2.02-fold and 25-fold selectivity for SHP2 over SHP1 and PTP1B respectively and had no visible activity against TCPTP. These preliminary results could provide a possible opportunity for the development of novel SHP2 inhibitors with optimal potency and improved pharmacological properties.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X17310582

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