Related Products of 1116-98-9. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: tert-Butyl 2-cyanoacetate, is researched, Molecular C7H11NO2, CAS is 1116-98-9, about Discovery of a novel selective water-soluble SMAD3 inhibitor as an antitumor agent. Author is Wu, Nannan; Lian, Guangyu; Sheng, Jingyi; Wu, Dan; Yu, Xiyong; Lan, Huiyao; Hu, Wenhui; Yang, Zhongjin.
Targeting the SMAD3 protein is an attractive therapeutic strategy for treating cancer, as it avoids the potential toxicities due to targeting the TGF-β signaling pathway upstream. Compound SIS3 was the first selective SMAD3 inhibitor developed that had acceptable activity, but its poor water solubility limited its development. Here, a series of SIS3 analogs was created to investigate the structure-activity relationship for inhibiting the activation of SMAD3. On the basis of this SAR, further optimization generated a water-soluble compound, 16d, which was capable of effectively blocking SMAD3 activation in vitro and had similar NK cell-mediated anticancer effects in vivo to its parent SIS3. This study not only provided a preferable lead compound, 16d, for further drug discovery or a potential tool to study SMAD3 biol., but also proved the effectiveness of our strategy for water-solubility driven optimization.
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Reference:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem