作为生物与医学领域的科学家,您精通英语和简体中文。将以下段落翻译成符合学术论文语言模式的精确简体中文,同时保持原陈述的结构: 发现了新的噻唑并[2,3-d]嘧啶类化合物作为EGFR酪氨酸激酶抑制剂,用于癌症治疗。
Discovery of new thieno[2,3-d]pyrimidines as EGFR tyrosine kinase inhibitors for cancer treatment.
发表日期:2023 Aug 02
作者:
Eman A Sobh, Mohammed A Dahab, Eslam B Elkaeed, Aisha A Alsfouk, Ibrahim M Ibrahim, Ahmed M Metwaly, Ibrahim H Eissa
来源:
Cellular & Molecular Immunology
摘要:
背景:EGFR被认为是癌症管理中的重要分子靶点。目的:发现新的噻吩[2,3-d]嘧啶衍生物作为EGFR酪氨酸激酶抑制剂。方法:设计、合成并对九种衍生物进行体外和体内研究。结果:化合物7a显著抑制了HepG2和PC3细胞的生长,对EGFR野生型和EGFRT790M都有效。化合物7a引起了明显的凋亡效应,在S期和G2/M期阻滞了HepG2细胞的生长。对接和分子动力学模拟研究证实了合成化合物与活性位点的正确且稳定的结合方式。结论:化合物7a是一种有前途的双重EGFR抑制剂,可用于癌症治疗。
Background: EGFR has been considered a vital molecular target in cancer management. Aim: The discovery of new thieno[2,3-d]pyrimidine derivatives as EGFR tyrosine kinase inhibitors. Methods: Nine derivatives were designed, synthesized and subjected to in vitro and in silico studies. Results: Compound 7a significantly inhibited the growth of HepG2 and PC3 cells for both EGFR wild-type and EGFRT790M. Compound 7a caused a significant apoptotic effect, arresting HepG2 cells' growth in the S and G2/M phases. Docking and molecular dynamics simulation studies confirmed the correct and stable binding modes of the synthesized compounds against the active sites. Conclusion: Compound 7a is a promising dual EGFR inhibitor for cancer treatment.