Cytotoxicity Evaluation of Dimethoxy and Trimethoxy Indanonic Spiroisoxazolines Against Cancerous Liver Cells

Abstract

Background: 3'-(3,4-dimethoxyphenyl)-4'-(4-(methylsulfonyl)phenyl)-4'H-spiro [indene-2,5'-isoxazol]-1(3H)-one and 4'-(4-(methylsulfonyl)phenyl)-3'-(3,4,5-trimethoxyphenyl)- 4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one compounds containing indanonic spiroisoxazoline core are widely known for their antiproliferative activities and investigation of tubulin binding modes. Objective: To evaluate the cytotoxicity effect of Dimethoxy and Trimethoxy Indanonic Spiroisoxazolines against HepG2 cancerous liver cell line and to perform a comparison with other known anti-liver cancer drugs. Methods: The evaluation of cytotoxicity of dimethoxy and trimethoxy indanonic spiroisoxazoline compounds, Oxaliplatin, Doxorubicin, 5-fluorouracil and Cisplatin against HepG2 (hepatocellular liver carcinoma) cell line has been performed using MTT assay and analyzed by GraphPad PRISM software (version 8.0.2). Results: Potent cytotoxicity effects against HepG2 cell line, comparable to Cisplatin (IC50= 0.047±0.0045 µM), Oxaliplatin (IC50= 0.0051µM), Doxorubicin (IC50= 0.0014µM) and 5- fluorouracil (IC50= 0.0089 µM), were shown by both dimethoxy (IC50= 0.059±0.012 µM) and trimethoxy (IC50= 0.086±0.019 µM) indanonic spiroisoxazoline compounds. Conclusion: In vitro biological evaluations revealed that dimethoxy and trimethoxy indanonic spiroisoxazoline compounds are good candidates for the development of new anti-liver cancer agents.

Synthesis of new spiroheterocycles-fused isoxazoline from 2-arylidenes-3-phenyl-1-indanones through a regio-and diastereospecific 1,3-dipolar cycloaddition

“…In addition, the spiroisoxazoline scaffold forms an integral part of many beneficial biologically active compounds. Indeed, spiroisoxazolines exhibit an extensive array of biological and pharmacological activities such as antiviral 13 , anticancer 14,17,18 , antimalarial 15 , antituberculosis 16 , antibacterial 17,19 and antiparasitic 20 .…”