1 research outputs found
Design, Synthesis, and Biological Evaluation of a Series of Anthracene-9,10-dione Dioxime β‑Catenin Pathway Inhibitors
The
Wnt/β-catenin signaling pathway plays a vital role in cell growth,
the regulation, cell development, and the differentiation of normal
stem cells. Constitutive activation of the Wnt/β-catenin signaling
pathway is found in many human cancers, and thus, it is an attractive
target for anticancer therapy. Specific inhibitors of this pathway
have been keenly researched and developed. Cell based screening of
compounds library, hit-to-lead optimization, computational and structure-based
design strategies resulted in the design and synthesis of a series
of anthracene-9,10-dione dioxime series of compounds demonstrated
potent inhibition of β-catenin in vitro (IC<sub>50</sub> <
10 nM, <b>14</b>) and the growth of several cancer cell lines.
This article discusses the potential of inhibiting the Wnt/β-catenin
signaling pathway as a therapeutic approach for cancer along with
an overview of the development of specific inhibitors