Ontology highlight
ABSTRACT:
SUBMITTER: Guo D
PROVIDER: S-EPMC9481106 | biostudies-literature | 2022 Dec
REPOSITORIES: biostudies-literature
Guo Dafeng D Yu Yu Y Long Binyu B Deng Ping P Ran Dongzhi D Han Lei L Zheng Jiecheng J Gan Zongjie Z
Journal of enzyme inhibition and medicinal chemistry 20221201 1
Simultaneous inhibition of histone deacetylases (HDACs) and anaplastic lymphoma kinase (ALK) could enhance therapeutic activity against ALK addicted cancer cells. Herein, a new series of 2,4-pyrimidinediamine derivatives as ALK and HDACs dual inhibitors were designed, synthesised and evaluated. Compound <b>12a</b> which possessed good inhibitory potency against ALK<sup>wt</sup> and HDAC1, exhibited stronger antiproliferative activity than Ceritinib on ALK positive cancer cell lines though induci ...[more]