Discovery of novel, potent and orally available benzoazipinone derivatives that elicit MKLP2-inhibitory phenotypes

Discovery of novel, potent and orally available benzoazipinone derivatives that elicit MKLP2-inhibitory phenotypes

Mitotic kinesin-like protein 2 (MKLP2/KIF20A) is a key mitotic regulator frequently overexpressed in human malignancies and its abundance is positively correlated with poor outcomes of the disease. Despite extensive research on MKLP2 as a potential target for oncology, the development of small-molec...

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Bibliographic Details
Main Authors: Jian Huang, Ting Zhang, Julia Kalashova, Jinhua Li, Chenglu Yang, Linsheng Zhong, Xiaohu Zhou, Qiong Shi, Gang Lv, Jiadai Chenyu, Yidan Xia Abuliezi, Duo Yu, Xuejiao Jiang, Mallu Chenna Reddy, Namrta Choudhry, Naganna Nimishetti, Dun Yang
Format: Article
Language:English
Published: Elsevier 2024-08-01
Series:European Journal of Medicinal Chemistry Reports
Subjects:
Mechanism-informed phenotypic screening
AURKB relocation
MKLP2
Benzoazipinone compounds
Tumor suppression
Online Access:http://www.sciencedirect.com/science/article/pii/S2772417424000177

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