AI Article Synopsis
- Ipomoeassin F, a macrolide from plants, effectively inhibits the growth of various cancer cell lines at low concentrations.
- Researchers created and tested 5-oxa/aza analogues for their cancer-fighting potential, discovering that modifying certain atoms slightly decreased efficacy but not significantly.
- Further experiments revealed that the size and flexibility of the chemical ring structure are critical for the bioactivity of ipomoeassin F.
Article Abstract
Ipomoeassin F, a plant-derived macrolide, exhibited single-digit nanomolar growth inhibition activity against many cancer cell lines. In this report, a series of 5-oxa/aza analogues was prepared and screened for cytotoxicity. Replacement of 5-CH with O/NH simplified the synthesis and led to only a small activity loss. N-methylation almost completely restored the potency. Further studies with additional 5-oxa analogues suggested, for the first time, that size and flexibility of the ring also significantly influence the bioactivity of ipomoeassin F.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5800971 | PMC |
| http://dx.doi.org/10.1016/j.ejmech.2017.11.022 | DOI Listing |
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New insights into structure-activity relationship of ipomoeassin F from its bioisosteric 5-oxa/aza analogues.
Eur J Med Chem
January 2018
Department of Chemistry and Biochemistry, J. William Fulbright College of Arts & Science, University of Arkansas, Fayetteville, AR, 72701, USA. Electronic address:
Article Synopsis
- Ipomoeassin F, a macrolide from plants, effectively inhibits the growth of various cancer cell lines at low concentrations.
- Researchers created and tested 5-oxa/aza analogues for their cancer-fighting potential, discovering that modifying certain atoms slightly decreased efficacy but not significantly.
- Further experiments revealed that the size and flexibility of the chemical ring structure are critical for the bioactivity of ipomoeassin F.
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