1135872-15-9Relevant articles and documents
Enantioconvergent and Regioselective Synthesis of Allenylsilanes by Nickel-Catalyzed C(sp2)-C(sp3) Cross-Coupling Starting from Racemic α-Silylated Propargylic Bromides
Xu, Yan,Yi, Hong,Oestreich, Martin
supporting information, p. 2194 - 2197 (2021/05/07)
A direct synthesis of enantioenriched allenylsilanes from racemic α-silylated propargylic bromides by an enantioconvergent nickel-catalyzed cross-coupling is reported. The high regioselectivity is governed by the bulky silyl group, and the C(sp2)-C(sp3) bond formation occurs exclusively at the γ-position of the propargyl electrophile. The level of enantioselection induced by a chiral Pybox ligand is moderate.
Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL
Sleebs, Brad E.,Kersten, Wilhemus J. A.,Kulasegaram, Sanji,Nikolakopoulos, George,Hatzis, Effie,Moss, Rebecca M.,Parisot, John P.,Yang, Hong,Czabotar, Peter E.,Fairlie, W. Douglas,Lee, Erinna F.,Adams, Jerry M.,Chen, Lin,Van Delft, Mark F.,Lowes, Kym N.,Wei, Andrew,Huang, David C.S.,Colman, Peter M.,Street, Ian P.,Baell, Jonathan B.,Watson, Keith,Lessene, Guillaume
supporting information, p. 5514 - 5540 (2013/07/26)
Developing potent molecules that inhibit Bcl-2 family mediated apoptosis affords opportunities to treat cancers via reactivation of the cell death machinery. We describe the hit-to-lead development of selective Bcl-X L inhibitors originating from a high-throughput screening campaign. Small structural changes to the hit compound increased binding affinity more than 300-fold (to IC50 w L. Surface plasmon resonance experiments afford strong evidence of binding affinity within the hydrophobic groove of Bcl-XL. Biological experiments using engineered Mcl-1 deficient mouse embryonic fibroblasts (MEFs, reliant only on Bcl-XL for survival) and Bax/Bak deficient MEFs (insensitive to selective activation of Bcl-2-driven apoptosis) support a mechanism-based induction of apoptosis. This manuscript describes the first series of selective small-molecule inhibitors of Bcl-XL and provides promising leads for the development of efficacious therapeutics against solid tumors and chemoresistant cancer cell lines.
Synthesis and properties of metal-ligand complexes with endohedral amine functionality
Johnson, Amber M.,Moshe, Orly,Gamboa, Ana S.,Langloss, Brian W.,Limtiaco, John F. K.,Larive, Cynthia K.,Hooley, Richard J.
, p. 9430 - 9442 (2011/11/04)
A series of tetracationic M2L4 palladium-pyridyl complexes with endohedral amine functionality have been synthesized. The complexes were analyzed by NMR techniques (including Diffusion NMR and 2D NOESY), electrospray ionization (ESI) mass spectrometry, and X-ray crystallography. The solid state analysis shows a large change in crystal morphology upon introduction of the endohedral amine groups, caused by deleterious interactions between the amines and the triflate counterions from the coordination process. Combination of different ligands allows analysis of ligand exchange rates via NMR analysis, with half-lives on the order of 3 h, independent of the donor properties of the ligand. Self-sorting behavior is observed, with more electron-rich ligands being favored. The amine-containing and extended complexes are strongly fluorescent, giving quantum yields of up to 83%.
BENZOTHIAZOLE COMPOUNDS
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Page/Page column 104, (2009/05/29)
The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival.
