6 research outputs found
Synthesis and conformational studies of α/β2,3-peptides derived from alternating β2,3-amino acids and L-Ala repeats
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Enantioselective synthesis of spliceostatin E and evaluation of biological activity.
An enantioselective total synthesis of spliceostatin E has been accomplished. The δ-lactone unit A was constructed from readily available (R)-glycidyl alcohol using a ring-closing olefin metathesis as the key reaction. A cross-metathesis of ring A containing δ-lactone and the functionalized tetrahydropyran B-ring provided spliceostatin E. Our biological evaluation of synthetic spliceostatin E revealed that it does not inhibit splicing in vitro and does not impact speckle morphology in cells. Spliceostatin E was reported to possess potent antitumor activity
ZrCl<sub>4</sub>-Catalyzed C-O Bond to C-N Bond Formation: Synthesis of 1,2,3-Triazoles and Their Biological Evaluation
<div><p></p><p>A simple and efficient protocol was developed for the synthesis of aryl azides directly from aryl carbinols using ZrCl<sub>4</sub> as a Lewis acid catalyst. The azides were converted to novel triazoles under click reaction conditions, which were evaluated for their antimicrobial activity against various strains.</p>
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Enantioselective Synthesis of Spliceostatin E and Evaluation of Biological Activity
An
enantioselective total synthesis of spliceostatin E has been
accomplished. The δ-lactone unit A was constructed from readily
available (<i>R</i>)-glycidyl alcohol using a ring-closing
olefin metathesis as the key reaction. A cross-metathesis of ring
A containing δ-lactone and the functionalized tetrahydropyran <i>B</i>-ring provided spliceostatin E. Our biological evaluation
of synthetic spliceostatin E revealed that it does not inhibit splicing
in vitro and does not impact speckle morphology in cells. Spliceostatin
E was reported to possess potent antitumor activity