4.5 Article

New antiproliferative 3-substituted oxindoles inhibiting EGFR/VEGFR-2 and tubulin polymerization

期刊

MOLECULAR DIVERSITY
卷 -, 期 -, 页码 -

出版社

SPRINGER
DOI: 10.1007/s11030-023-10603-z

关键词

Antiproliferative activity; Receptor tyrosine kinases (RTKs); Tubulin polymerization inhibitors; 3-Substituted oxindole; MCF-7; Molecular-docking studies

向作者/读者索取更多资源

New 3-substituted oxindole derivatives were synthesized and evaluated as antiproliferative agents. Among the tested compounds, compounds 6f and 6g showed remarkable antiproliferative activity against leukemia and breast cancer cell lines. Compound 6f exhibited the most promising antiproliferative activity against MCF-7 (human breast cancer), and inhibited receptor tyrosine EGFR and tubulin polymerization.
New 3-substituted oxindole derivatives were designed and synthesized as antiproliferative agents. The antiproliferative activity of compounds 6a-j was evaluated against 60 NCI cell lines. Among these tested compounds, compounds 6f and 6g showed remarkable antiproliferative activity, specifically against leukemia and breast cancer cell lines. Compound 6f was the most promising antiproliferative agent against MCF-7 (human breast cancer) with an IC50 value of 14.77 mu M compared to 5-fluorouracil (5FU) (IC50 = 2.02 mu M). Notably, compound 6f hampered receptor tyrosine EGFR fundamentally with an IC50 value of 1.38 mu M, compared to the reference sunitinib with an IC50 value of 0.08 mu M. Moreover, compound 6f afforded anti-tubulin polymerization activity with an IC50 value of 7.99 mu M as an outstanding observable activity compared with the reference combretastatin A4 with an IC50 value of 2.64 mu M. In silico molecular-docking results of compound 6f in the ATP-binding site of EGFR agreed with the in vitro results. Besides, the investigation of the physicochemical properties of compound 6f via the egg-boiled method clarified good lipophilicity, GIT absorption, and blood-brain barrier penetration properties.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.5
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据