Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 2-Chloronicotinoyl chloride, is researched, Molecular C6H3Cl2NO, CAS is 49609-84-9, about Discovery of [1,2,4]triazolo[4,3-a]pyridines as potent Smoothened inhibitors targeting the Hedgehog pathway with improved antitumor activity in vivo.Recommanded Product: 2-Chloronicotinoyl chloride.
Twenty [1,2,4]triazolo[4,3-a]pyridines I (R = C6H5, 2-ClC6H4, 2-Cl,4-FC6H3, etc,) were designed, synthesized and screened as Smoothened (Smo) inhibitors. Four of these novel compounds exhibited directly bound to Smo protein with stronger binding affinity than Vismodegib (VIS). The new compounds exhibited broad anti-proliferative activity against cancer cell lines in vitro, especially triple-neg. breast cancer cells. Mechanistic studies demonstrated that I (R = 2,6-di-Cl-pyridine) markedly induced cell cycle arrest and apoptosis in MDA-MB-468 cells. Compound I (R = 2,6-di-Cl-pyridine) blocked Smo translocation into the cilia and reduced Smo protein and mRNA expression. Furthermore, the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1) was significantly inhibited. Finally, I (R = 2,6-di-Cl-pyridine) demonstrated greater anti-tumor activity in authors’ animal models than VIS with lower toxicity. Hence, these results support further optimization of this novel scaffold to develop improved Smo antagonists.
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Reference:
Phosphine ligand,
Chiral phosphine ligands in asymmetric synthesis. Molecular structure and absolute configuration of (1,5-cyclooctadiene)-(2S,3S)-2,3-bis(diphenylphosphino)butanerhodium(I) perchlorate tetrahydrofuran solvate