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New Approach for Tetrachlorosilane Promoted One-Pot, Condensation Reaction for Tetrahydrobenzo[a]Xanthene-11-Ones with Docking Validation as Aurora Kinase Inhibitor

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Abstract

An efficient synthesis is reported for tetrahydrobenzo[a]xanthene-11-ones through a one-pot catalytic reaction by mixing β-naphthol, demidone and aromatic aldehydes in the presence of a catalytic amount of tetrachlorosilane (TCS) in methylene chloride as solvent at ambient temperature compared with other catalysts derived from silicon. Aurora kinase inhibitors have attracted a great deal of interest as a new class of antimitotic agents and so the molecular docking study was carried out on the synthesized compounds compared with pentacyclic AKI-001 to discover a novel class of Aurora inhibitors based on a tetracyclic xanthene scaffold and understand the orientation and the interaction of each molecule inside the active site of the Aurora A enzyme.

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Correspondence to Tamer K. Khatab.

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Soliman, H.A., Khatab, T.K. New Approach for Tetrachlorosilane Promoted One-Pot, Condensation Reaction for Tetrahydrobenzo[a]Xanthene-11-Ones with Docking Validation as Aurora Kinase Inhibitor. Silicon 10, 229–233 (2018). https://doi.org/10.1007/s12633-016-9421-0

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  • DOI: https://doi.org/10.1007/s12633-016-9421-0

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