Small-molecule activation

Ru-catalyzed Suzuki-type cross-coupling reactions of aniline derivatives and organoboronates have been achieved via unreactive aryl C—N bond cleavage (Equation 11.48) [109]. The proposed reaction pathway is a sequence of oxidative addition of an unreactive aryl C—N bond to the late transition metal complex, followed by transmetalation between the Ru-NR2 species and organoboronates, and reductive elimination. [Pg.359]

H2 is the simplest molecule, consisting of two protons and two electrons. Because its oxidation leads to water as the sole product, it has been regarded as a clean proton source. In many industrially important reactions, such as hydroformylation and hydrogenation, dihydrogen gas serves as a reducing agent or H-atom source. The BDE of H2 is I 103.25(1) kcal mol 1 [111], Therefore, H2 is an unreactive molecule. [Pg.359]

Transition metals are the main promoters for H—H bond cleavage assisted by the coordination of o- H—H bond to metal atoms. An example is presented here. The reaction of low-coordinate L3Fe-([x-N)-FeL3 complexes and H2 generates Fe(p.-NH) (q-H)Fe species under mild conditions (Equation 11.49) [112]. [Pg.359]

Significantly, stable singlet carbenes could mimic the transition metals for H2 activation under mild conditions (Equation 11.50) [113]. Mechanistically, in contrast to transition metals that act as electrophiles towards H2, the carbenes behave as nucleophiles. As a result, this nucleophilic behavior also allows carbenes to activate N H3. [Pg.360]

In addition, a heterolytic cleavage of H2 was achieved via the cooperation of B (C6Fs)3 and amines (Equation 11.51) [114]. As an application, benzaldehyde is reduced by the present system. [Pg.360]

Tripodal Carbene and Aryloxide Ligands for Small-Molecule Activation at Electron-Rich Uranium and Transition Metal Centers Karsten Meyer and Suzanne C. Bart... [Pg.655]

Kang, J., Chen, X.L., Wang, H., Ji, J., Cheng, H., Incardona, J., Reynolds, W., Viviani, F., Tabart, M. and Rampe, D. (2005) Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Molecular Pharmacology, 67, 827-836. [Pg.106]

TRIPODAL CARBENE AND ARYLOXIDE LIGANDS FOR SMALL-MOLECULE ACTIVATION AT ELECTRON-RICH URANIUM AND TRANSITION METAL CENTERS... [Pg.1]

II. Synthesis and Characterization of Ligand Precursors and Low-Valent Metal Complexes for Small-Molecule Activation... [Pg.1]

III. Small-Molecule Activation A. Reactivity of [(TIMEN )Co] Complexes... [Pg.15]

Several small molecule modulators (SMM) of p300 and PCAF have been developed (Varier et al, 2004). Recently, the first naturally occurring HAT inhibitor anacardic acid was isolated from cashew nut shell liquid, which inhibits the HAT activity of both p300 and PCAF very effectively (Balasubramanyam et al, 2003). By using anacardic acid as a synthon, an amide derivative of anacardic acid, CTPB, has been synthesized, which is the only known small molecule activator of any histone acetyltransferase, in this case, p300. However, cells are impermeable or... [Pg.278]

Varier RA, Swaminathan V, Balasubramanyam K, Kundu TK (2004) Implications of small molecule activators and inhibitors of histone acetyltransferases in chromatin therapy. Biochem Pharmacol... [Pg.292]

Small molecule activators of sirtuins extend Saccharomyces cere-visiae lifespan. Nature 425 191-196. [Pg.165]

Cohen, H.Y., Lamming, D.W., Lavu, S., Wood, J.G. et al. (2003) Small molecule activators of sirtuin expan Saccharomyces cerevisiae lifespan. Nature, 425,191-196. [Pg.84]

Small molecule activators of SIRTl as therapeutics for the treatment of type 2 diabetes. Nature, 450, 712-716. [Pg.241]

This well-established process of inference via similarity is not without error every once in a while the bioinformatics-based inference of protein function will be incorrect. Much more frequently, the cheminformatics-based inference of small molecule activity is in error, since slight changes in a molecule can dramatically affect its ability to bind. Hence, in cheminformatics, inference of function from similarity classification is less reliable than in bioinformatics. Because of this lack of reliability, inference in cheminformatics is thought of as an imperfect screening process, whose less than ideal performance is analyzed in terms of an enrichment factor (a measure of how much better the cheminformatic inference performs than random inference). [Pg.159]

S. Basu, B. Ellinger, S. Rizzo, C.l. Deraeve, M. Schurmann, H. Preut, H.-D. Arndt, and H. Waldmann, Biology-oriented synthesis of a natural-product inspired oxepane. Collection yields a small-molecule activator of the Wnt-pathway, Proc. Natl. Acad. Sci. USA., 108 (2011) 6805-6810. [Pg.186]

Howitz KT, Bitterman KJ, Cohen HM, Lamming DH, Lavu S, Wood JG, Zipkin RE, Chung P, Kisielewski A, Zhang L-L, Scherer B, Sinclair DA. 2003. Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan. Nature 425 191-196. [Pg.210]

Transcellular transport Basic mechanisms of transepithelial transport of drugs include passive transport of small molecules, active transport of ionic and polar compounds, and endocytosis and transcytosis of macromolecules. [Pg.532]

HEAVY ATOM ISOTOPE EFFECTS AS PROBES OF SMALL MOLECULE ACTIVATION... [Pg.426]

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