Institute of Plant Science, ARO, Volcani Center, Rishon LeZion, 7505101, Israel.
Adichunchanagiri Institute for Molecular Medicine, Nagamangala, Karnataka, 571448, India.
Chem Biodivers. 2020 May;17(5):e2000014. doi: 10.1002/cbdv.202000014. Epub 2020 Apr 16.
An efficient, metal free approach to synthesize multi-substituted Δ -pyrroline derivatives by mild base catalyzed cyclocondensation of malononitrile with Erlenmeyer azlactones via 1,2 addition was developed. The modularity of this reaction was used to assemble a range of poly-substituted pyrrolines. Further, synthesized products were screened for cytotoxic properties on different cancer cell lines such as A549 (Human lung adenocarcinoma cells), HeLa (Human cervical adenocarcinoma cells), Jurkat (Human chronic myeloid leukemia cells) and K562 (Human leukemic T cell Lymphoblast cells). Among the synthesized library of compounds, 6f and 6q displayed potent cytotoxic activity.
发展了一种高效、无金属的方法，通过温和碱催化的丙二腈与 Erlenmeyer 氮杂内酯的 1,2 加成环缩合，合成了多取代的Δ-吡咯啉衍生物。该反应的模块性被用于组装一系列多取代的吡咯啉。此外，对合成的产物在不同的癌细胞系（如 A549（人肺腺癌细胞）、HeLa（人宫颈癌细胞）、Jurkat（人慢性髓性白血病细胞）和 K562（人白血病 T 细胞淋巴母细胞））上进行了细胞毒性筛选。在所合成的化合物库中，化合物 6f 和 6q 表现出很强的细胞毒性活性。
