Yu, Yu; Ran, Dongzhi; Jiang, Junhao; Pan, Tao; Dan, Yanrong; Tang, Qiang; Li, Wei; Zhang, Lin; Gan, LinLing; Gan, Zongjie published the artcile< Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2>, Electric Literature of 2382-10-7, the main research area is purin derivative preparation anticancer HDAC CDK dual inhibitor; Antitumor; CDKs; Dual inhibitors; HDACs; Purin.
HDAC and CDK inhibitors have been demonstrated to be synergistically in suppressing cancer cell proliferation and inducing apoptosis. In this work, we incorporated the pharmacophore groups of HDACs and CDKs inhibitors into one mol. to design and synthesize a series of purin derivatives as HDAC/CDK dual inhibitors. The lead compound I, showing good HDAC1 and CDK2 inhibitory activity with IC50 values of 5.8 and 56 nM, resp., exhibited attractive potency against several cancer cell lines in vitro. This work may lead to the discovery of a novel scaffold and potential dual HDAC/CDK inhibitors.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Electric Literature of 2382-10-7.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics