Abstract
Novel analogues of (+)-varitriol have been synthesised via Julia-Kocienski olefination from -Dribonolactone. Newly prepared compounds were screened for their in vitro cytotoxicity towards certain human tumours and NCI60 cancer cell line panel.
Highlights
Marine fungi are an important source of marine natural products.[1]
As a part of our ongoing project in the synthesis of new polyhydroxylated tetrahydrofurans as potential antitumour agents from monosaccharides,[15] we have recently developed a short and effective synthesis of varitriol from -D-ribonolactone.7c we wish to report the synthesis of varitriol analogues and their antitumour activity
Chemistry The array of interesting biological properties of (+)-1 and the unknown mode of its action motivated us to synthesise a variety of analogues and to examine the bioactivity of structurally diverse „varitriol-like“ compounds against set of tumour cell lines
Summary
Marine fungi are an important source of marine natural products.[1]. Recently, the four new compounds, (+)-varitriol 1, varioxirane 2, dihydroterrein 3, and varixanthone 4 have been isolated[2] from a marine-derived strain of the fungus Emericella variecolor (Figure 1). Final removal of the acetonide and acetyl protecting group with 1M aqueous HCl in THF and NaOMe in MeOH, respectively, furnished target compounds 6a-k, 7a-k as the mixtures of E/Z-isomers (Table 1), which were separated by preparative MPLC.
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