Oxidative regioselective amination of chromones exposes potent inhibitors of the hedgehog signaling pathway.
نویسندگان
چکیده
A transition metal-free, oxidative, regioselective cross-coupling between non-functionalized azoles and chromones at C2-position was developed. A broad reaction scope and further transformation of products were demonstrated. The biological evaluation of products revealed a novel class of hedgehog signaling pathway inhibitors.
منابع مشابه
The role of the desert hedgehog signaling pathway during degeneration and regeneration of peripheral nerves
The desert hedgehog (Dhh) signaling pathway is involved in the development of peripheral nerves (PNs). Dhh-null mice show abnormal neuronal development and perineurial barrier function. As it was previously shown that dhh is mainly expressed in developmental nerves and Sonic hedgehog protein (dhh homologous) has therapeutic effects in neuronal survival, we attempted to investigate the possible ...
متن کاملThe role of the desert hedgehog signaling pathway during degeneration and regeneration of peripheral nerves
The desert hedgehog (Dhh) signaling pathway is involved in the development of peripheral nerves (PNs). Dhh-null mice show abnormal neuronal development and perineurial barrier function. As it was previously shown that dhh is mainly expressed in developmental nerves and Sonic hedgehog protein (dhh homologous) has therapeutic effects in neuronal survival, we attempted to investigate the possible ...
متن کاملInvestigating the role of signaling pathways and cancer stem cells in esophageal cancer with a therapeutic approach
Esophageal cancer (EC) is the sixth main cause of cancer death worldwide. Important genes associated with esophageal cancer include FOXO3, AKT, and GSK3β. Excessive FOXO3 expression inhibits the proliferation of cancer cells. The expression of AKT is involved in controlling cell growth in tumors. GSK3β activity is higher in cancer tissues. Given the effective role of cancer stem cells (CSCs) in...
متن کاملRole of Oxidative Stress in Modulating Unfolded Protein Response Activity in Chronic Myeloid Leukemia Cell Line
Background: Recently, it has been revealed that tyrosine kinase inhibitors (TKIs) act through inducing both oxidative and endoplasmic reticulum (ER) stress in chronic myeloid leukemia cells. However, ER stress signaling triggers both apoptotic and survival processes within cells. Nevertheless, mechanisms by which TKIs avoid the pro-survival effects are not clear. The aim of this study was to ev...
متن کاملDesign and Evolution of a Macrocyclic Peptide Inhibitor of the Sonic Hedgehog/Patched Interaction.
The hedgehog (Hh) signaling pathway plays a central role during embryonic development, and its aberrant activation has been implicated in the development and progression of several human cancers. Major efforts toward the identification of chemical modulators of the hedgehog pathway have yielded several antagonists of the GPCR-like smoothened receptor. In contrast, potent inhibitors of the sonic...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Chemical communications
دوره 51 5 شماره
صفحات -
تاریخ انتشار 2015