Novel Diphenylamine 2,4'-Dicarboxamide Based Azoles as Potential Epidermal Growth Factor Receptor Inhibitors: Synthesis and Biological Activity

DOI Web Site Web Site PubMed 被引用文献1件 参考文献24件

この論文をさがす

説明

Several hybrid molecules of diphenylamine-2,4′-dicarboxamide with various azolidinones and related heterocyclic rings have been synthesized and explored as epidermal growth factor receptor (EGFR) kinase inhibitors. Most of them displayed promising in vitro tyrosine kinase inhibition as well as potent cellular antiproliferative activity in the EGFR over-expressing breast cancer cell line (MCF-7). Compounds 12b and 13b that exhibited the highest inhibition in the kinase assay (89, 81% inhibition at 10 μM, respectively), showed potent antiproliferative effect against MCF-7 tumor cell line (IC50 1.04, 0.91 μM respectively). Molecular docking studies revealed that these compounds can bind to ATP binding site of the EGFR kinase domain and were involved in H-bonding with Met 793, in analogy to the known EGFR tyrosine kinase inhibitors. Moreover, compounds 15a—c possessed profound antitumor activity (IC50 0.59—0.73 μM) and significant EGFR-TK inhibition, making them of particular interest. In summary, the newly synthesized compounds provide promising new lead for the future design and development of anticancer agents of potential EGFR-TK inhibitory activity.

収録刊行物

被引用文献 (1)*注記

もっと見る

参考文献 (24)*注記

もっと見る

キーワード

詳細情報 詳細情報について

問題の指摘

ページトップへ