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Updated: Jun 21, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis, antimalarial activity and cytotoxicity of substituted 3,6-diphenyl-[1,2,4,5]tetraoxanes
Nitin Kumar1, Shabana I Khan, Beena
1Department of Chemistry, University of Delhi, Delhi 110 007, India.
Abstract:
Substituted tetraoxanes with different substitution pattern on the aromatic ring were synthesized in order to explore the influence of different substituents in the antimalarial activity. Antimalarial activity of these compounds improves by the introduction of ethyl, iso-propyl or n-propyl groups in the aromatic ring but substitution with n-butyl or t-butyl leads decrease in antimalarial activity. Some of these compounds exhibit promising antimalarial activity. None of the compounds shows any toxicity against vero cells and three compounds (2a-2c) were tested against panel of six cell lines and none of these compounds showed any toxicity. X-ray crystal structure of compound 2w showed that tetraoxane ring is in the chair conformation with both the phenyl rings in the equatorial position. In addition, FeCl(3) mediated O-O bond scission of tetraoxanes (2a-2c) was also examined.
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