444020-06-8Relevant academic research and scientific papers
Stereoselective synthesis of a potent human NK1 receptor antagonist via acyl-Claisen rearrangement
Raubo, Piotr,Giuliano, Claudio,Hill, Alastair W.,Huscroft, Ian T.,London, Clare,Reeve, Austin,Seward, Eileen M.,Swain, Christopher G.,Kulagowski, Janusz J.
, p. 600 - 604 (2007/10/03)
Stereoselective synthesis of the tetrahydropyran derivative 1 is reported. Diastereoselective acyl-Claisen rearrangement was employed for formation of C3 and C4 chiral centres on the tetrahydropyran ring. Georg Thieme Verlag Stuttgart.
Synthesis and MMP-inhibitory activity of gelastatin analogues
Cho, Ju-Hee,Ko, Soo Y.,Oh, Eugene,Park, Jae C.,Yoo, Ji U.
, p. 3994 - 3999 (2007/10/03)
Gelastatin A and B, isolated from culture broth of Westerdykella multispora F 50733, have been reported to exhibit MMP-inhibitory activities at a sub-micromolar level. In an effort to exploit this lead, we synthesized gelastatin analogues in which the conjugated triene unit of natural gelastatins was replaced by the benzylidene group. The (Z)-isomeric synthetic benzylidene-gelastatin exhibited MMP-inhibitory activities comparable to those reported for the natural products. Therefore, this compound appears to be a viable lead in searching for therapeutically useful MMP inhibitors.
