[EN] MCL-1 MODULATING COMPOSITIONS<br/>[FR] COMPOSITIONS DE MODULATION DE MCL-1
申请人:PENN STATE RES FOUND
公开号:WO2013112878A1
公开(公告)日:2013-08-01
The present invention relates to marinopyrrole A derivatives and pyoluteorin derivatives and methods of treatment of disorders associated with misregulation of Mcl-l, e.g., leukemia, lymphoma, multiple myeloma, melanoma, or pancreatic cancer. We describe exemplary compounds, which may be contained in pharmaceutical compositions, and their use as therapeutic agents either alone or in combination with other anti-cancer treatments, e.g., anti-Bcl- 2 agents.
Asymmetric synthesis and anti-protozoal activity of the 8,4′-oxyneolignans virolin, surinamensin and analogues
作者:Claire E. Rye、David Barker
DOI:10.1016/j.ejmech.2012.12.013
日期:2013.2
The asymmetric synthesis of 8,4′-oxyneolignans (−)-virolin, (−)-surinamensin and a number of analogues has been achieved. A divergent synthesis was used, with all compounds being elaborated from a single chiral aldehyde derived from ethyl lactate. In the 15 compounds that were tested, the level of substitution on the A-ring was found to directly influence the activity against Leishmania donovani whilst
Rearrangements of aryl-8-oxabicyclo[3.2.1]octenones: synthesis of novel biaryls and 1-aryl-3-furylpropanones
作者:John Mann、Philip D. Wilde、Mark W. Finch
DOI:10.1039/c39850001543
日期:——
The formation of 3-arylbenzaldehydes through rearrangement of 3-aryl-8-oxabicyclo[3.2.1]oct-2-en-7-ones is reported, together with various rearrangement reactions of 2-aryl-8-oxabicyclo[3.2.]oct-6-en-3-ones, and a novel approach to the natural product acamelin.
Regioselective difunctionalization of arenes remains a long-standing challenge in organic chemistry. We report a novel and general Fe/Ti synergistic methodology for regioselective synthesis of various polysubstituted arenes through either E/E′ or Nu/E ortho difunctionalizations of arenes. Preliminary results showed that an unprecedented 1,2-Fe/Ti heterobimetallic arylene intermediate bearing two distinct