Yang, Yang published the artcileStructure-activity relationship study of DEL-22379: ERK dimerization inhibitors with increased safety, Synthetic Route of 104-01-8, the main research area is lung liver cancer DEL22379 anticancer agent ERK signaling; Anti-cancer activity; ERK dimerization inhibitor; Indolin-2-one; Structure–activity relationship; Synthesis.
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].
Molecular Diversity published new progress about Albumins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Synthetic Route of 104-01-8.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem