Shallal, Hassan M.; Russu, Wade A. published the artcile< Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives>, SDS of cas: 374930-88-8, the main research area is piperazinylpyrimidine derivative preparation antitumor activity breast carcinoma kinase profiling.
Protein kinases play several pertinent roles in cell proliferation, and targeting these proteins has been shown to be a successful strategy toward controlling different malignancies. Despite the great discovery stories during the last two decades, there is still a demand for anticancer small mols. with the potential of being selective on both the protein kinase and/or the cellular level. A series of novel piperazinylpyrimidine compounds was synthesized and the members tested for their potential to selectively inhibit the growth of certain tumor cell lines included within the NCI-60 cell line panel. MDA-MB-468, a triple-neg./basal-like breast carcinoma cell line was among the most sensitive cell lines towards compounds I and II. The three most interesting compounds identified in cellular screens (I, II, and III) were subjected to kinase profiling and found to have an interesting selective tendency to target certain kinase subfamily members; PDGFR, CK1, RAF and others. Compound I showed a selective tendency to bind to and/or inhibit the function of certain KIT and PDGFRA mutants compared to their wild-type isoforms. Piperazinylpyrimidine based derivatives represent a new class of selective kinase inhibitors. Significantly, I is more potent at inhibiting oncogenic mutant forms of PDGFR family kinases, which is relevant in terms of its potential use in treating tumors that have become resistant to treatment or driven by such mutations. The clin. demand for agents useful in the control of triple-neg./basal-like breast cancer justifies interest in compound II which is a potent growth inhibitor of MDA-MB-468 cell line.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, SDS of cas: 374930-88-8.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics