Abstract：
Aim: Synthesis of pyrazole derivatives as EGFR inhibitors. Materials & methods: Cytotoxicity and EGFR inhibitory effect were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and EGFR kits, respectively. The biodistribution of radioiodinated compound nanoparticles in tumor-bearing mice was studied. Results: The IC50 values of compound 4a against HepG2 cells and EGFR were 0.15 ± 0.03 and 0.31 ± 0.008 μM, respectively, while those of erlotinib were 0.73 ± 0.04 and 0.11 ± 0.008 μM, respectively. The binding scores of compound 4a and erlotinib to EGFR were -9.52 and -10.23 Kcal/mol, respectively. The maximum tumor uptake of radioiodinated compound after intravenous nanoparticle injection was 6.7 ± 0.3% radioactivity/g. Conclusion: Compound 4a is a promising antitumor agent with a potential EGFR inhibitory effect.
摘要：
目的:EGFR抑制剂吡唑衍生物的合成。材料和方法：通过3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四唑溴化物和EGFR试剂盒评估细胞毒性和EGFR抑制作用，分别。研究了放射性碘化化合物纳米颗粒在荷瘤小鼠中的生物分布。结果:化合物4a对HepG2细胞和EGFR的IC50值分别为0.15±0.03和0.31±0.008μM,分别,而厄洛替尼的剂量为0.73±0.04和0.11±0.008μM，分别。化合物4a和埃罗替尼与EGFR的结合评分分别为-9.52和-10.23Kcal/mol,分别。静脉内纳米颗粒注射后放射性碘化化合物的最大肿瘤摄取为6.7±0.3%放射性/g。结论:化合物4a是一种具有潜在EGFR抑制作用的有前途的抗肿瘤药物。
