Aim: Literature reports suggest spirochromanone derivatives exhibit anticancer activity. Methodology: The authors designed and synthesized 18 spirochromanone derivatives (Csp 1-18). The compounds were characterized and evaluated for anticancer activity against human breast cancer (MCF-7) and murine melanoma (B16F10) cell lines. Results: The anticancer activity ranged from 4.34 to 29.31 μm. The most potent compounds, Csp 12 and Csp 18, were less toxic against the human embryonic kidney (HEK-293) cell line and ∼ two/∼four fold selective toward MCF-7 than B16F10 in comparison to the reference, BG-45. Csp 12 caused 28.6% total apoptosis, leading to significant cytotoxicity, and arrested the G2 phase of the cell cycle in B16F10 cells. A molecular docking study of Csp 12 exhibited effective binding at the active site of the epidermal growth factor receptor kinase domain. Conclusion: This study highlights the importance of spirochromanones as anticancer agents.

Design, synthesis and structure-activity relationship studies of novel spirochromanone hydrochloride analogs as anticancer agents.

A Review on Chemical and Biological Studies of 4-Chromanone Derivatives

3-Chloro-3-chlorosulfenyl-4′-methylspiro[chroman-2,1′-cyclohexane]-4-one (4) was prepared from the reaction of spiro 4′-methylcyclohexan-1′,2-chroman-4-one (3) with thionyl chloride according to re...

Tamer El Malah

Papers

Chemical and anticancer activity studies for some 3-chloro-3-chlorosulfenyl-4′-methylspiro[chroman-2,1′-cyclohexane]-4-ones