2-Aminobenzimidazole
cores are among the most common structural
components in medicinal chemistry and can be found in many biologically
active molecules. Herein, we report a mild protocol for the synthesis
of multifunctional 2-aminobenzimidazoles on-DNA with broad substrate
scopes. The reaction conditions expand our ability to design and synthesize
2-aminobenzimidazole core-focused DNA-encoded libraries.
A series of novel histone deacetylase (HDAC) inhibitors were designed, synthesized and evaluated based on the strategies of a hybrid of the classic pharmacophore of HDAC inhibitors with the thiazolidinone scaffold. Some of the compounds 12i showed potent HDAC1 inhibition with nM IC50 values, more importantly, compound displayed much better anti-metastatic effects than vorinostat (SAHA) against migration of the A549 cell line. Further mechanism exploration implied that compound 12i may inhibit tumor metastasis via modulating the epithelial-mesenchymal transition (EMT) and upregulating the acetylation of α-tubulin.
Hemostasis is a major challenge in surgical procedures and traumas. Conventional hemostatic methods have limited efficacy and may cause additional tissue damage. In this study, we designed a novel hemostatic agent based on the in situ gel formation of gelatin cross-linked by a novel microbial transglutaminase (mTGase), in which the amino acid sequences differed from commercial mTGases. The new hemostatic agent showed the same biochemical crosslinking chemistry as the final stages of the blood coagulation cascade while using gelatin as a "structural" protein (rather than fibrin) and a calcium-independent mTGase as the crosslinking catalyst (rather than factor XIIIa). In rat liver hemostasis models, the hemostatic agent not only showed a similar hemostatic effect as that of SURGIFLO (positive control), but also stronger adhesion strength and elasticity than SURGIFLO. Therefore, this biomimetic gelatin-mTGase mix hemostatic is a novel and effective surgical sealant.
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