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通过胺结诺素衍生物向抑制口腔状细胞癌的向抑制

Asmita Choithramani¹, Rudradip Das¹, Gourav Bothra¹

¹Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research-Ahmedabad (NIPER-A) Opposite Airforce Station, Palaj Gandhinagar Gujarat - 382355 India amit@niperahm.res.in.

RSC medicinal chemistry

|August 16, 2024

概括

研究人员开发了新的昆素结合的伊米达索皮里米丁衍生物作为潜在的口腔癌 (OC) 疗法. 化合物12d通过激活pyruvate kinase M2 (PKM2) 对OC细胞表现出强大的抗癌活性.

科学领域:

药用化学医学化学
在瘤学瘤学.
分子生物学分子生物学

背景情况:

口腔癌 (OC) 仍然是全球癌症死亡的主要原因.
目前的治疗方法在延长患者存活时间方面具有有限的有效性.
迫切需要针对OC的新型治疗策略.

研究的目的:

设计和合成新的昆素结合的伊米达索皮里米丁衍生物.
为了评估这些化合物的体外抗癌活性与OC细胞系对比.
为了研究最强效化合物的作用机制.

主要方法:

合成了二十五种新的昆素结合的伊米达索皮里米丁衍生物.
在体外细胞毒性测定使用CAL-27 (OC) 和正常口腔上皮细胞 (NOE) 细胞系.
细胞循环分析,亡试验,in silico对接和酶活性试验 (PKM2激活).

主要成果:

化合物12d对OC细胞表现出强烈的抗增殖活性 (IC50 = 0.79μM),对NOE细胞的毒性最小.
12d诱导了S阶段细胞周期停止,并在OC细胞中促进了细胞亡.
在体研究中证实了12d与PKM2的结合,酶测定表明12d是一种强大的PKM2激活剂 (AC50 = 0.6nM).

结论:

合成的昆素结合的伊米达索皮里米丁衍生物显示出作为治疗口腔癌的新型抗癌剂的前景.
化合物12d通过向PKM2.2,显示出作为治疗剂的巨大潜力.
这项研究为开发新的OC治疗提供了坚实的基础.

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