The dual FAK-HDAC inhibitor MY-1259 displays potent activities in gastric cancers in vitro and in vivo
J Song, X Liu, YF Zhang, XY Tian, MY Deng… - Bioorganic …, 2023 - Elsevier
Epigenetic regulation and Focal adhesion kinase (FAK) are considered to be two important
targets for the development of antitumor drugs. Studies have shown that the combination of …
targets for the development of antitumor drugs. Studies have shown that the combination of …
Design, synthesis and biological evaluation of novel 2, 4-diaminopyrimidine cinnamyl derivatives as inhibitors of FAK with potent anti-gastric cancer activities
Y Liu, LJ Kong, N Li, YH Liu, MQ Jia, QG Liu… - Bioorganic …, 2023 - Elsevier
In this study, twenty-one novel 2, 4-diaminopyrimidine cinnamyl derivatives as inhibitors
targeting FAK were designed and synthesized based on the structure of TAE-226, and the …
targeting FAK were designed and synthesized based on the structure of TAE-226, and the …
A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1, 2, 4-triazoles
Abstract Novel 5-pyridinyl-1, 2, 4-triazoles were designed as dual inhibitors of histone
deacetylase 2 (HDAC2) and focal adhesion kinase (FAK). Compounds 5d, 6a, 7c, and 11c …
deacetylase 2 (HDAC2) and focal adhesion kinase (FAK). Compounds 5d, 6a, 7c, and 11c …
Design, synthesis and biological evaluation of novel FAK inhibitors with better selectivity over IR than TAE226
T Chen, Y Liu, J Liu, M Tang, H Huang, C Bai, W Si… - Bioorganic …, 2022 - Elsevier
In this study, 28 novel focal adhesion kinase (FAK) inhibitors were designed and
synthesized based on FAK inhibitor TAE226. Compound 18b displayed good inhibition of …
synthesized based on FAK inhibitor TAE226. Compound 18b displayed good inhibition of …
Discovery of 7H-pyrrolo [2, 3-d] pyridine derivatives as potent FAK inhibitors: Design, synthesis, biological evaluation and molecular docking study
R Wang, X Zhao, S Yu, Y Chen, H Cui, T Wu, C Hao… - Bioorganic …, 2020 - Elsevier
Focal adhesion kinase (FAK) is an intracellular non-receptor tyrosine kinase responsible for
development of various tumor types. Aiming to explore new potent inhibitors, two series of 2 …
development of various tumor types. Aiming to explore new potent inhibitors, two series of 2 …
Discovery of novel pyrrolo [2, 3-d] pyrimidine derivatives as potent FAK inhibitors based on cyclization strategy
S Zeng, S Yuan, Y Zhang, J Du, Y Wu, Y Chen… - Bioorganic …, 2023 - Elsevier
Focal adhesion kinase (FAK), a non-receptor tyrosine kinase, plays a pivotal role in tumor
invasion and metastasis. Many FAK inhibitors had been reported, but the development of …
invasion and metastasis. Many FAK inhibitors had been reported, but the development of …
A synergistic anticancer FAK and HDAC inhibitor combination discovered by a novel chemical–genetic high-content phenotypic screen
JC Dawson, B Serrels, A Byron, MT Muir… - Molecular cancer …, 2020 - AACR
We mutated the focal adhesion kinase (FAK) catalytic domain to inhibit binding of the
chaperone Cdc37 and ATP, mimicking the actions of a FAK kinase inhibitor. We …
chaperone Cdc37 and ATP, mimicking the actions of a FAK kinase inhibitor. We …
Design, synthesis, biological evaluation and molecular docking study of novel thieno [3, 2-d] pyrimidine derivatives as potent FAK inhibitors
R Wang, S Yu, X Zhao, Y Chen, B Yang, T Wu… - European Journal of …, 2020 - Elsevier
Abstract A series of 2, 7-disubstituted-thieno [3, 2-d] pyrimidine derivatives were designed,
synthesized and evaluated as novel focal adhesion kinase (FAK) inhibitors. The novel 2, 7 …
synthesized and evaluated as novel focal adhesion kinase (FAK) inhibitors. The novel 2, 7 …
A small molecule focal adhesion kinase (FAK) inhibitor, targeting Y397 site: 1-(2-hydroxyethyl) -3, 5, 7-triaza-1-azoniatricyclo [3.3.1.1 3,7 ]decane; bromide …
VM Golubovskaya, S Figel, BT Ho, CP Johnson… - …, 2012 - academic.oup.com
Focal adhesion kinase (FAK) is a protein tyrosine kinase that is overexpressed in most solid
types of tumors and plays an important role in the survival signaling. Recently, we have …
types of tumors and plays an important role in the survival signaling. Recently, we have …
Discovery of antiproliferative and anti-FAK inhibitory activity of 1, 2, 4-triazole derivatives containing acetamido carboxylic acid skeleton
M Mustafa, GEDA Abuo-Rahma… - Bioorganic & medicinal …, 2021 - Elsevier
Small molecule inhibitors of the focal adhesion kinase are regarded as promising tools in
our armamentarium for treating cancer. Here, we identified four 1, 2, 4-triazole derivatives …
our armamentarium for treating cancer. Here, we identified four 1, 2, 4-triazole derivatives …
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