当前位置: X-MOL 学术Bioorgan. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
A new class of diamide scaffold: Design, synthesis and biological evaluation as potent antimitotic agents, tubulin polymerization inhibition and apoptosis inducing activity studies.
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2018-12-05 , DOI: 10.1016/j.bioorg.2018.12.007
Khaled O Mohamed 1 , Islam Zaki 2 , Ibrahim M El-Deen 3 , Mohammed K Abdelhameid 1
Affiliation  

A new series of diamide functional compounds has been designed, synthesized and confirmed by spectroscopic methods and elemental analyses. All the synthesized compounds were evaluated for their antiproliferative activity on HepG2 cell line. Compounds 3k and 3l were proved to have potent anticancer activity equipotent or more potent than reference compound Combretastatin A-4. The results of DNA flow cytometry analysis demonstrated cell cycle arrest at G2/M phase. The extent of apoptosis induced by 3k and 3l was also determined. Moreover, the compounds produced a significant reduction in cellular microtubules for microtubule loss and potently inhibited the binding of [3H]colchicine to tubulin. Compounds 3k and 3l were proved to upregulate expression of proteins triggering apoptosis, such as p53, Bax, and decreased Bcl-2 overexpression as well as increased the expression of effector caspase- 3/7.

中文翻译:

一类新型的二酰胺支架:作为有效的抗有丝分裂剂的设计,合成和生物学评估,微管蛋白聚合抑制和细胞凋亡诱导活性研究。

通过光谱方法和元素分析,设计,合成和确认了一系列新的二酰胺功能化合物。评价所有合成的化合物对HepG2细胞系的抗增殖活性。化合物3k和3l被证明具有比参考化合物Combretastatin A-4等效的或更有效的抗癌活性。DNA流式细胞仪分析的结果表明细胞周期停滞在G2 / M期。还确定了3k和3l诱导的细胞凋亡程度。此外,该化合物使细胞微管的微管损失显着减少,并有效抑制[3H]秋水仙碱与微管蛋白的结合。化合物3k和3l被证明可以上调触发细胞凋亡的蛋白质的表达,例如p53,Bax,
更新日期:2018-12-05
down
wechat
bug