881683-81-4Relevant articles and documents
CALPAIN MODULATORS AND METHODS OF PRODUCTION AND USE THEREOF
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, (2017/09/27)
The present technology relates to compounds, kits, compositions, and methods useful for the treatment of fibrotic disease. In some aspects, the present technology provides for treatment of various diseases or disorders associated or mediated, at least in part, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is generally applicable to compounds which inhibit myofibroblast differentiation.
A concise synthesis of the HCV protease inhibitor BILN 2061 and its P3 modified analogs
Liu, Dejun,Dong, Jingchao,Yin, Yunxing,Ma, Rujian,Shi, Yifeng,Wu, Hao,Chen, Shuhui,Li, Ge
, p. 1489 - 1502 (2011/11/01)
A concise synthesis of BILN 2061 was achieved through more efficient installation of P2 4-quinoline moiety via SN2 displacement of the β-OBs group located on the 4-hydroxyl proline intermediate, which was prepared from 4-α-hydroxyl proline analog via Mitsunobu reaction with inversion of stereochemistry. In addition, a short and practical synthesis for P3 unit is also described herein. Final assembly of four fragments for BILN 2061 was achieved with an overall yield of 58% in 4 steps from P1 to 15a. Furthermore several analogs of BILN 2061 (WX-1-WX-5) containing modifications on P3 unit were synthesized successfully using the same synthetic route as described for the parent inhibitor BILN 2061. Copyright
Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides
Nishino, Norikazu,Shivashimpi, Gururaj M.,Soni, Preeti B.,Bhuiyan, Mohammed P.I.,Kato, Tamaki,Maeda, Satoko,Nishino, Tomonori G.,Yoshida, Minoru
, p. 437 - 445 (2008/09/16)
Inhibitors of histone deacetylases (HDACs) are a promising class of anticancer agents that effect gene regulation. To know the interaction of aliphatic cap groups with HDACs, cyclic tetrapeptide and bicyclic peptide disulfide hybrids were synthesized without aromatic ring in their macrocyclic framework. Benzene ring of l-Phe in chlamydocin was replaced with several aliphatic amino acids and also a fused bicyclic tetrapeptide was synthesized by ring closing metathesis using Grubb's first generation catalyst. The inhibitory activities of the cyclic peptides against histone deacetylase enzymes were evaluated, which demonstrated most of them are interesting candidates as anticancer agents.
A NOVEL PROCESS FOR THE PREPARATION OF NONRACEMIC LONG CHAIN α-AMINO ACIDS DERIVATIVES
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Page/Page column 21; 24 - 25, (2008/06/13)
The present invention provides a process for the preparation of a nonracemic a-amino acid derivative from an optically active N-acyl lactam using an organometallic reagent to effect the opening of the ring followed by reduction of the ketone carbonyl to an alcohol or a methylene, or by a reductive amination to an amine, or by a ketalization reaction.