비소세포폐암 세포주 H1975에 대한 2-아닐리노피리미딘 구조 기반 선택적 저해제의 발견 연구

• 영문명: Discovery of 2-Anilinopyrimidine-based Selective Inhibitors against Non-small Cell Lung Cancer Cell Line H1975
• 발행기관: 대한약학회
• 저자명: 이진영 김소현 김승태 김희규 응웬후롱 정영석 윤화영
• 간행물 정보: 『약학회지』제66권 제6호(2022년), 345~349쪽, 전체 5쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2022.12.30

영문 초록

Small molecular EGFR-tyrosine kinase inhibitors (EGFR-TKIs) have been proved as a successful and powerful strategy for the treatment of non-small-cell lung cancer (NSCLC). Recent studies have reported that the T790M mutation in EGFR is the most prevalent factor in acquired resistance for NSCLC patients. In an effort to identify small molecules for the inhibition of T790M mutant EGFR, a screening of our in-house chemical library was conducted by an MTT assay. A set of 2-anilinopyrimidine derivatives was rationally selected and then evaluated for their antiproliferative activities against three different type of NSCLC cell lines H358 (EGFR wild-type), HCC827 (EGFR exon 19 deletion) and H1975 (EGFR L858R/T790M double-mutant). Compounds 9, possessing a piperidine in the part A and a 4-methylpiperidine in the part B, selectively showed inhibitory activity in the T790M mutant cell line. In addition, in silico studies of 9 utilizing a SwissADME tool exhibited good drug-like properties.

목차

서론(Introduction)

방법(Methods)

결과 및 고찰(Results and Discussion)

결론(Conclusion)

감사의 말씀(Acknowledgment)

Conflict of Interest

References

키워드

2-Anilinopyrimidine NSCLC EGFR T790M In-house chemical library