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비소세포폐암에서 Gefitinib 내성 극복을 위한 효과적인 화합물 합성 및 항암 활성 평가
김광일(Kwang Il Kim),박소연(So-Yeon Park),최대옥(Daeock Choi),김항건(Hangun Kim) 대한약학회 2024 약학회지 Vol.68 No.2
Lung cancer remains a leading cause of global cancer-related mortality, emphasizing the need for innovative strategies to combat resistance to the first-generation EGFR tyrosine kinase inhibitors (EGFR-TKIs), Gefitinib. This study aimed to discover and evaluate small molecule compounds selectively inhibiting Gefitinib resistance. A compound library was screened against adenocarcinoma (A549), EGFR-mutant NSCLC (H1975 and PC9), and Gefitinib-resistant NSCLC (PC9GR) cell lines. The study identified W1 as a promising lead compound, and its derivative, compound W3, exhibited excellent efficacy in PC9 and PC9GR cells. These findings underscore the potential of W3, an 4-anilinopyrimidine derivative, as an inhibitor of Gefitinib resistance in NSCLC. This research contributes valuable insights to the ongoing efforts in developing effective and sustainable treatment options for lung cancer patients facing EGFR-TKI resistance.
Choi, Daeock 순천대학교 기초과학연구소 1997 基礎科學硏究誌 Vol.8 No.-
Functionalized amino acid derivatives (2) were studied whether these can serve as new agents for the treatment of peripheral nervous system (PNS) disorders. Recently evidence has been presented that the commercial antiepileptic agent, phenytoin, was effective in pharmacological tests designed to model PNS diseases.^4 Accordingly, polar derivatives of 2 were synthesized and then evaluated both for central nervous system (CNS) and PNS activity using the MES-seizure and the acetic acid writhing tests, respectively. In this study, it was reasoned that polar derivatives of 2 might be selective to the PNS since they would be unlikely to cross the blood-brain barrier.