SIS3, a good candidate for the reverse of type 2 diabetes mellitus in mice.

TGF-β signaling plays an extremely important role in the occurrence and development of type 2 diabetes mellitus (T2DM), and the blockade of TGF-β/Smad3 pathway protests against the high-fat diet-induced obesity and diabetes. As a specific small molecule inhibitor of Smad3 protein, the biological activities of compound SIS3 were evaluated by high-fat diet-induced T2DM model mice. In vivo results indicated that SIS3 can not only significantly reduce the body weight, fat mass, and fasting blood glucose in high-fat diet-induced T2DM model mice, but also improve insulin sensitivity and oral glucose tolerance of high-fat diet-induced T2DM model mice after the injection of SIS3 with 5 mg/kg for 45 days.

Synthesis and biological evaluation of novel benzamide derivatives as potent smoothened antagonists.

A series of novel benzamide derivatives were prepared and evaluated using cell-based measurements. Among these compounds, 10f significantly inhibited Hedgehog signaling and showed equivalent or more potency than GDC-0449 in different tests. Furthermore, compound 10f potently inhibited the proliferation of Daoy, a medulloblastoma cell line that is reported to be resistant to GDC-0449, which indicated a promising prospect in the treatment of Hedgehog signaling pathway related cancer in clinical trial.

6-Amino-2-methyl-8-phenyl-1,2,3,4-tetra-hydro-iso-quinoline-5,7-dicarbo-nitrile.

In the title compound, C18H16N4, the dihedral angle between the benzene and phenyl rings is 61.40 (4)°. In the crystal, mol-ecules are linked by N-H⋯N(nitrile) hydrogen bonds, forming inversion dimers.

2-Chloro-N-(4-chloro-3-iodo-phen-yl)-4-(methyl-sulfon-yl)benzamide.

In the title compound, C(14)H(10)Cl(2)INO(3)S, the dihedral angle between the benzene rings is 52.13 (10)°. In the crystal, the components are linked by pairs of N-H⋯O(sulfon-yl) hydrogen bonds into centrosymmetric dimers.