비소세포폐암에서 Gefitinib 내성 극복을 위한효과적인 화합물 합성 및 항암 활성 평가

• Published in: Yaghag-hoi-ji pp. 94 - 97
• Main Authors: 김광일, 박소연, 최대옥, 김항건
• Format: Journal Article
• Language: Korean
• Published: 대한약학회 01.04.2024
• Subjects: 약학
• ISSN: 0377-9556; 2383-9457
• DOI: 10.17480/psk.2024.68.2.94

Lung cancer remains a leading cause of global cancer-related mortality, emphasizing the need for innovativestrategies to combat resistance to the first-generation EGFR tyrosine kinase inhibitors (EGFR-TKIs), Gefitinib. This studyaimed to discover and evaluate small molecule compounds selectively inhibiting Gefitinib resistance. A compound librarywas 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, exhibitedexcellent efficacy in PC9 and PC9GR cells. These findings underscore the potential of W3, an 4-anilinopyrimidinederivative, as an inhibitor of Gefitinib resistance in NSCLC. This research contributes valuable insights to the ongoingefforts in developing effective and sustainable treatment options for lung cancer patients facing EGFR-TKI resistance. KCI Citation Count: 0