Arienti, Kristen L. published the artcileCheckpoint Kinase Inhibitors: SAR and Radioprotective Properties of a Series of 2-Arylbenzimidazoles, Name: 4-(4-Chlorophenoxy)benzaldehyde, the main research area is checkpoint kinase inhibitor radioprotective arylbenzimidazole structure activity relationship.
The discovery of a series of novel, potent, and highly selective inhibitors of the DNA damage control kinase chk2 is disclosed. Here we report the first SAR study around inhibitors of this kinase. High-throughput screening of purified human chk2 led to the identification of a novel series of 2-arylbenzimidazole inhibitors of the kinase. Optimization was facilitated using homol. models of chk2 and docking of inhibitors, leading to the highly potent 2-arylbenzimidazole 2h (IC50 15 nM). Compound 2h is an ATP-competitive inhibitor of chk2 that dose dependently protects human CD4+ and CD8+ T-cells from apoptosis due to ionizing radiation. This work suggests that a selective small mol. inhibitor of chk2 could be a useful adjuvant to radiotherapy, increasing the therapeutic window of such treatment.
Journal of Medicinal Chemistry published new progress about Apoptosis. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Name: 4-(4-Chlorophenoxy)benzaldehyde.
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics