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NIR-emitting benzothiazolium cyanines with an enhanced stokes shift for mitochondria imaging in live cells
10.1039/C8OB00327K 2018-04-11 A series of benzothiazolium-based hemicyanines (3a–3f) have been synthesized. Evaluation of their photophysical properties shows that they exhibit improved photophysical characteristics. In comparison with the available commercial MitoTrackers, the new probes... |
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Stability and anti-inflammatory activity of the reduction-resistant curcumin analog, 2,6-dimethyl-curcumin
10.1039/C8OB00639C 2018-04-11 The efficacy of the curry spice compound curcumin as a natural anti-inflammatory agent is limited by its rapid reductive metabolism in vivo. A recent report described a novel synthetic derivative, 2,6-dimethyl-curcumin, with increased stability against reduct... |
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Recent Progress of Heavy Atom-Free Organic Compounds Showing Unexpected Intersystem Crossing (ISC) Ability
10.1039/C8OB00421H 2018-04-11 In this review, the recent progress of the heavy atom-free triplet photosensitizers was summarized. The general approaches include to attain S1/Tn states sharing similar energy levels, or proper molecular geometry to satisfy the reservation of the angular mom... |
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Beyond geminal diesters: increasing the scope of metal-mediated vinylcyclopropane annulations while decreasing pre-activation
10.1039/C8OB00593A 2018-04-11 The utilization of unactivated substrates in annulation reactions provides access to complex products without the need for subsequent removal of the activating group. Vinylcyclopropanes (VCPs), occurring naturally in several monoterpene natural products, are ... |
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Stereodivergent Synthesis of 5-Aminopipecolic Acids and Application in the Preparation of a Cyclic RGD Peptidomimetic as a Nanomolar αVβ3 Integrin Ligand
10.1039/C8OB00534F 2018-04-11 A stereodivergent strategy was devised to obtain enantiopure cis and trans 5-aminopipecolic acids (5-APAs) in suitably protected forms to be employed in peptide synthesis as conformationally constrained α- and δ-amino acids. The cis isomer was used as a δ-ami... |
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NFSI-participated intermolecular aminoazidation of alkene through iron catalysis
10.1039/C8OB00699G 2018-04-11 An iron-catalysed intermolecular vicinal aminoazidation of alkenes, using N-fluorobenzenesulfonimide (NFSI) and trimethylsilyl azide (TMSN3) as the imidating and azidating reagents, respectively, is described, which could potentially provide a valuable route ... |
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One-Pot Synthesis of 1,5-Diketones from 3-acetyl-4-Hydroxycoumarin and Effective Cyclization to Unexpected 3, 4-dihydropyridines
10.1039/C8OB00718G 2018-04-11 A facile synthesis of 1, 5-diketones from 3-acetyl-4-hydroxycoumarin, aldehydes and cyclic-ketones via a one-pot aldol condensation and subsequent Michael addition reaction in presence of a single catalyst of L-proline under mild reaction condition has been d... |
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Realisation of small molecule libraries based on frameworks distantly related to natural products
10.1039/C8OB00688A 2018-04-11 The availability of high-quality screening compounds is of paramount importance for the discovery of innovative new medicines. Natural product (NP) frameworks can inspire the design of productive compound libraries. Here, we describe the design and synthesis ... |
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A transition state “trapped”? QM-cluster models of engineered threonyl-tRNA synthetase
10.1039/C8OB00540K 2018-04-10 In a recent study [Science, 2015, 347, 6224], protein engineering was used to design a core within the enzyme threonyl-tRNA synthetase (ThrRS) capable of stabilizing the coplanar transition state conformation of an inserted noncanonical p-biphenylalanine (BiP... |
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Synthesis of a C-functionalized TE1PA and comparison with analogues. Example of bioconjugation on 9E7.4 mAb for multiple myeloma 64Cu-PET imaging
10.1039/C8OB00499D 2018-04-10 According to the excellent copper(II) and 64-copper(II) complexation of TE1PA ligand, a monopicolinate cyclam, in both aqueous medium and in vivo, we looked for a way to make it bifunctional, while keeping intact its chelating properties. Overcoming the alrea... |