Abstract
(Chemical Equation Presented) Highly convergent syntheses of eight phorboxazole congeners and their evaluation against a diverse panel of human solid tumor cancer cell lines have been achieved. Specifically, the C(45-46) alkyne, alkene, and alkane phorboxazole A analogues [(+)-4-(+)-6] were constructed and found to display single digit nanomolar cell growth inhibitory activities in a series of human cancer cell lines. The structurally simplified C(11-15)-acetal congener (+)-20Z also proved potent albeit reduced (cf. 34.6 nM) when evaluated against the same cell line panel. Importantly, (+)-C(46)-chlorophorboxazole A (3) displayed picomolar (pM) inhibitory activity in several cell lines.
Original language | English (US) |
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Pages (from-to) | 1201-1208 |
Number of pages | 8 |
Journal | Journal of Organic Chemistry |
Volume | 73 |
Issue number | 4 |
DOIs | |
State | Published - Feb 15 2008 |
ASJC Scopus subject areas
- Organic Chemistry