Journal
MOLECULAR DIVERSITY
Volume 27, Issue 2, Pages 845-855Publisher
SPRINGER
DOI: 10.1007/s11030-022-10458-w
Keywords
Hybrid molecule; Cytotoxicity; HCT-116; Akt1 inhibitor; Molecular docking
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A series of hybrid compounds were synthesized and their antiproliferative activity against tumor cells was evaluated. Promising compounds were found to selectively inhibit specific cell lines, suggesting potential molecular mechanisms.
A series of dihydrofuran-3-one and 9,10-phenanthrenequinone hybrid compounds were synthetized through a one-pot gold-catalyzed oxidative cyclization and Aldol-type addition cascade reaction of homopropargylic alcohols with 9,10-phenanthrenequinone. The cytotoxicity of newly synthesized compounds was evaluated in CCK8 assay against different human cancer cells, showing significantly antiproliferative activity against tested tumor cell lines with a lowest IC50 value of 0.92 mu M over HCT-116. Further investigation revealed that the treatment of HCT-116 cell line with the promising compound 4c induced cell death as a selective Akt inhibitor. In addition, controlled experiments and molecular docking study suggested that the significant antitumor activity might be attributed to the unique hybrid structure, which implied the promising potential of this dual heterocycle hybrid method in the discovery of novel bioactive molecules with structural diversity. [GRAPHICS] .
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