Synthesis and conformational studies of α/β2,3-peptides derived from alternating β2,3-amino acids and L-Ala repeats

International audienc

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

ZrCl₄-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 ZrCl₄ 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> </div

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