Design, synthesis and biological evaluation of novel FAK inhibitors with better selectivity over IR than TAE226

Chen, Tao; Liu, Yan; Liu, Jiang; Tang, Minghai; Huang, Hao; Bai, Chunmei; Si, Wenting; Yang, Xue; Wen, Yi; Chen, Lijuan

doi:10.1016/j.bioorg.2022.105790

Cited by 9 publications

(1 citation statement)

References 38 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In addition, 12 counteracted clone formation, HCT-116 cell migration and HUVEC tube formation; furthermore, this compound caused cell cycle arrest in the G2/M phase, causing apoptosis by promoting reactive oxygen species (ROS) production and blocking the FAK-Src-ERK (Extracellular signal-regulated kinases) signalling pathway in a dose-dependent manner. Moreover, 12 was endowed with good oral bioavailability and inhibited tumor growth in the HCT116 xenograft model [ 37 ].…”

Section: Fak Inhibitorsmentioning

confidence: 99%

The Development of FAK Inhibitors: A Five-Year Update

Spallarossa

Tasso

Russo

et al. 2022

IJMS

View full text Add to dashboard Cite

Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase over-expressed in different solid cancers. In recent years, FAK has been recognized as a new target for the development of antitumor agents, useful to contrast tumor development and metastasis formation. To date, studies on the role of FAK and FAK inhibitors are of great interest for both pharmaceutical companies and academia. This review is focused on compounds able to block FAK with different potencies and with different mechanisms of action, that have appeared in the literature since 2017. Furthermore, new emerging PROTAC molecules have appeared in the literature. This summary could improve knowledge of new FAK inhibitors and provide information for future investigations, in particular, from a medicinal chemistry point of view.

show abstract

Section: Fak Inhibitorsmentioning

confidence: 99%