Issue 50, 2020

Synthesis and biological evaluation of fluoro-substituted spiro-isoxazolines as potential anti-viral and anti-cancer agents

Abstract

Electrophilic fluorine-mediated dearomative spirocyclization has been developed to synthesize a range of fluoro-substituted spiro-isoxazoline ethers and lactones. The in vitro biological assays of synthesized compounds were probed for anti-viral activity against human cytomegalovirus (HCMV) and cytotoxicity against glioblastomas (GBM6) and triple negative breast cancer (MDA MB 231). Interestingly, compounds 4d and 4n showed significant activity against HCMV (IC50 ∼ 10 μM), while 4l and 5f revealed the highest cytotoxicity with IC50 = 36 to 80 μM. The synthetic efficacy and biological relevance offer an opportunity to further drug-discovery development of fluoro-spiro-isoxazolines as novel anti-viral and anti-cancer agents.

Graphical abstract: Synthesis and biological evaluation of fluoro-substituted spiro-isoxazolines as potential anti-viral and anti-cancer agents

Supplementary files

Article information

Article type
Paper
Submitted
14 7月 2020
Accepted
06 8月 2020
First published
17 8月 2020
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2020,10, 30223-30237

Synthesis and biological evaluation of fluoro-substituted spiro-isoxazolines as potential anti-viral and anti-cancer agents

P. Das, S. Boone, D. Mitra, L. Turner, R. Tandon, D. Raucher and A. T. Hamme, RSC Adv., 2020, 10, 30223 DOI: 10.1039/D0RA06148D

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