Synthesis of Novel Quin[1,2-b]Acridines: In Vitro Cytotoxicity and Molecular Docking Studies

• Published in: Polycyclic aromatic compounds Vol. 41; no. 8; pp. 1631 - 1645
• Main Authors: Satheeshkumar, Rajendran, Edatt, Lincy, Muthusankar, Aathi, Sameer Kumar, V. B., Rajendra Prasad, Karnam Jayarampillai
• Format: Journal Article
• Language: English
• Published: Taylor & Francis 14-09-2021
• Subjects: 2,3-Dihydroacridin-4(1H)-ones; Cytotoxic activity; Molecular docking studies; Quin[1,2-b]acridines
• ISSN: 1040-6638; 1563-5333
• DOI: 10.1080/10406638.2019.1689515

An attempted synthesis of 5-aryl-6,7-dihydrodibenzo[b,j][1,10]phenanthroline derivatives from 2,3-dihydroacridin-4(1H)-ones with 2-aminocarboxylic acid derivatives in presence of phosphorus oxychloride at 130˚C yielded a novel class of quin[1,2-b]acridine derivatives. The newly synthesized compounds showed a better cytotoxic activity against HeLa and MCF-7 cell lines during the structure-activity relationship (SAR) studies. To discover with the interactions of these molecules, we carried out molecular docking studies using the human protein kinase CK2 inhibitors. The molecular interaction results provided a number of elegant information for the outlook design of more potent inhibitors.