Yang, Yang; Zhou, Yuanzheng; Tao, Lei; Yang, Tao; Zhao, Yinglan; Luo, Youfu published the article 《Structure-activity relationship study of DEL-22379: ERK dimerization inhibitors with increased safety》. Keywords: lung liver cancer DEL22379 anticancer agent ERK signaling; Anti-cancer activity; ERK dimerization inhibitor; Indolin-2-one; Structure–activity relationship; Synthesis.They researched the compound: 1-Piperidineacetic Acid( cas:3235-67-4 ).Name: 1-Piperidineacetic Acid. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:3235-67-4) here.
Abstract: Aberrant activation of ERK signaling pathway usually leads to oncogenesis, and small mol. agents targeting this pathway are impeded by the emergence of drug resistance due to reactivation of ERK signaling. Compound DEL-22379 has been reported to inhibit ERK dimerization which was unaffected by drug-resistant mechanism reactivating the ERK signaling. Here, we discussed a structure-activity relationship study of DEL-22379. Forty-seven analogs were designed and synthesized. Each synthesized compound was biol. evaluated for their inhibitory rates on several tumor cell lines and compounds with high inhibitory rates were further evaluated for IC50 values. The structure-activity relationship of idolin-2-one scaffold and the impact of Z/E configuration on potency were discussed. Potential safety of two synthesized analogs was investigated and in silico docking study of five compounds was performed to understand the structural basis of ERK dimerization inhibition. Graphic abstract: [graphic not available: see fulltext].
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