Integrating a phenotypic screening with a structural simplification strategy to identify 4-phenoxy-quinoline derivatives to potently disrupt the mitotic localization of Aurora kinase B.

doi:10.1016/j.bmc.2023.117173

Article

Integrating a phenotypic screening with a structural simplification strategy to identify 4-phenoxy-quinoline derivatives to potently disrupt the mitotic localization of Aurora kinase B.

Bioorganic & medicinal chemistry - 15 Feb 2023

Lv Gang, Shi Qiong, Zhang Ting, Li Jinhua, Long Yan, Zhang Wenhui, Choudhry Namrta, Yang Kevin, Li Hongmei, Kalashova Julia, Yang Chenglu, Zhou Xiaohu, Reddy Mallu Chenna, Anantoju Kishore Kumar, Zhang Shenqiu, Zhang Jing, Allen Thaddeus D, Liu Hong, Nimishetti Naganna, Yang Dun

Abstract excerpt

We combined a mechanism-informed phenotypic screening (MIPS) assay with a structural simplification strategy to guide the discovery of compounds that disrupt the localization of the mitotic regulator, Aurora kinase B (AURKB), rather than inhibiting its catalytic activity. An initial hit 4-(4-methylthiophen-2-yl)-N-(4-(quinolin-4-yloxy)phenyl)phthalazin-1-amine was identified after screening an in-house library of...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Aurora Kinase A

Integrating a phenotypic screening with a structural simplification strategy to identify 4-phenoxy-quinoline derivatives to potently disrupt the mitotic localization of Aurora kinase B.

Abstract excerpt

Topics

Related research