952577-78-5Relevant articles and documents
Synthesis and activity of bivalent FKBP12 ligands for the regulated dimerization of proteins
Keenan, Terence,Yaeger, David R.,Courage, Nancy L.,Rollins, Carl T.,Pavone, Mary Ellen,Rivera, Victor M.,Yang, Wu,Guo, Tao,Amara, Jane F.,Clackson, Tim,Gilman, Michael,Holt, Dennis A.
, p. 1309 - 1335 (1998)
The total synthesis and in vitro activities of a series of chemical inducers of dimerization (CIDs) is described. The use of small-molecule CIDs to control the dimerization of engineered FKBP12-containing fusion proteins has been demonstrated to have broad utility in biological research as well as potential medical applications in gene and cell therapies. The facility and flexibility of preparation make this new class of wholly synthetic compounds exceptionally versatile tools for the study of intracellular signaling events mediated by protein-protein interactions or protein localization. While some congeners possess potency comparable to or better than the first generation natural product-derived CID, FK1012, structure-activity relationships are complex and underscore the need for application-specific compound optimizations. Copyright (C) 1998 Elsevier Science Ltd.
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines
Ansari, Farzana Latif,Iftikhar, Fatima,Ihsan-ul-Haq,Mirza, Bushra,Baseer, Mohammad,Rashid, Umer
, p. 7691 - 7697 (2008/12/23)
Solid-phase synthesis of a parallel library of 3′-hydroxy-2,3-dihydrobenzothiazepines has been carried out through [4+3] annulation of α,β-unsaturated ketones with aminothiophenol, using Wang resin as solid support. The synthesized compounds were evaluated for their potential as antibacterial, tumor inhibitors as well as acetyl- and butyrylcholinesterase inhibitors. None of the compounds showed any significant antibacterial activity. However, quite a few compounds showed significant potential as crown gall tumor inhibitors. These results reflect a strong exploratory potential in search of new benzothiazepines as source of anticancer agents. The results of the inhibition of cholinesterase revealed that benzothiazepines have a greater potential as butyrylcholinesterase inhibitors as compared to acetylcholinesterase. Moreover, the substitution of hydroxy group at C-3 in ring A led to increased activity when compared to unsubstituted- and 2′-OH substituted benzothiazepines.