Home
Resources
Publications
Efficient Synthesis of New Phenanthridine Wnt/β-catenin Signaling Pathway Agonists

Efficient Synthesis of New Phenanthridine Wnt/β-catenin Signaling Pathway Agonists

Duozhi Chen, Heng Zhang, Chenxu Jing, Xiaoli He, Bijuan Yang, Jieyun Cai, Yunfu Zhou, Xiaoming Song, Lin Li, Xiaojiang Hao

Eur J Med Chem. 2018 Sep 5;157:1491-1499.

PMID: 30282321

Abstract:

Previously, HLY78, a lycorine derivative, was identified as the first Wnt/β-catenin signaling agonist through binding to the DAX domain of Axin, a scaffold of Wnt/β-catenin complex. In this study, to obtain more potent Wnt/β-catenin agonist, the structure optimization of HLY78 was carried out by design and synthesis of six phenanthridine derivatives, which afforded five active ones. In particular, 8,9-bis((1,3-dimethyl-1H-pyrazol)methoxy)-5-ethyl-4-methyl-5,6-dihydrophenanthridine showed the most potent activity (0.15/μM) that was increased nearly 30 times as that of the lead HLY78. These compounds may be valuable in future pharmacological or biological studies.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP854847613	HLY78		854847-61-3	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: