Grindstone Chemistry: Design, One-Pot Synthesis, and Promising Anticancer Activity of Spiro[acridine-9,2′-indoline]-1,3,8-trione Derivatives Against the MCF-7 Cancer Cell Line

• Main Authors: Perumal Gobinath, Ponnusamy Packialakshmi, Ali Daoud, Saud Alarifi, Akbar Idhayadhulla, Surendrakumar Radhakrishnan
• Format: Article
• Language: English
• Published: MDPI AG 2020-12-01
• Series: Molecules
• Subjects: isatin; indole; solvent-free conditions; cyclocondensation; grinding; p-TSA catalyst
• Online Access: https://www.mdpi.com/1420-3049/25/24/5862
• ISSN: 1420-3049

In this study, the synthesis of one-pot 10-phenyl-3,4,6,7-tetrahydro-1<i>H</i>-spiro [acridine-9,2′-indoline]-1,3,8-trione derivatives was achieved via a four-component cyclocondensation reaction, which was carried out in solvent-free conditions, and using p-toluenesulfonic acid (p-TSA) as a catalyst. The product was confirmed by FT-IR, ¹H-NMR, ¹³C-NMR, mass spectra, and elemental analysis. Furthermore, the anticancer activity was screened for all compounds. Among these compounds, compound <b>1c</b> was more effective (GI₅₀ 0.01 µm) against MCF-7 cancer cell lines than standard and other compounds. Therefore, the objective of this study was achieved with a few promising molecules having been demonstrated to be potential anticancer agents.