经过实践和使用简便的Mn(OAc)2促进的[3+2]环加成反应，使得烯酮胺与异氰基乙酸酯反应，产生了多样性的3-芳酰吡咯-2-羧酸酯，反应涵盖了广泛的底物。新合成的化合物大多数在四种癌细胞中显示出适度的抗增殖活性。值得注意的是，化合物2n在四种不同的癌细胞系中显示出最高的活性，平均IC50值为5.61 μM。此外，2n还表现出有利的抗迁移活性和类药物特性。进一步的研究表明，2n具有抑制ERK5活性的能力，并与ERK5蛋白结合，使其成为新型ERK5抑制剂发现领先化合物的有前景的候选物。版权所有©2023 Elsevier Inc. 保留所有权利。

The practical and facile Mn(OAc)2-promoted [3+2] cycloaddition reaction of enaminones with isocyanoacetate was developed, that delivered a diversity of 3-aroyl pyrrole-2-carboxylic esters with broad substrates scope. The most of the newly synthesized compounds exhibit moderate antiproliferative activity against four cancer cells. Notably, compound 2n demonstrate the most potent activity with average IC50 values of 5.61 μM against four distinct cancer cell lines. Moreover, 2n exhibit favorable anti-migration activity and drug-like properties. The further investigation suggests that compound 2n possesses the ability to inhibit ERK5 activity and exhibits effective binding with the ERK5 protein, making it a promising candidate as a lead compound for a new class of ERK5 inhibitors discovery.Copyright © 2023 Elsevier Inc. All rights reserved.