- Synthesis of calamitic, liquid crystalline porphyrins with lateral aromatic branches
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The lateral, electron-accepting aromatic substituent was successfully used to obtain a conformationally pure, laterally substituted liquid crystalline porphyrin. In addition, the attempt to synthesize a strapped, rod-like porphyrin showed that the planarity of the porphyrin core could be crucial in molecular design to synthesize strapped liquid crystalline porphyrin.
- Wang, Qing Min,Bruce, Duncan W.
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Read Online
- How Far Can We Push the Rigid Oligomers/Polymers toward Ferroelectric Nematic Liquid Crystals?
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The emerging ferroelectric nematic (NF) liquid crystal is a novel 3D-ordered liquid exhibiting macroscopic electric polarization. The combination of the ultrahigh dielectric constant, strong nonlinear optical signal, and high sensitivity to the electric f
- Aya, Satoshi,Cen, Fangjie,Dai, Shuqi,Huang, Houbing,Huang, Mingjun,Jiang, Yuanbin,Kougo, Junichi,Lei, Huanyu,Li, Jinxing,Xia, Runli,Xu, Hao,Yang, Jidan,Zhang, Guangzu,Zhang, Xinxin
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supporting information
p. 17857 - 17861
(2021/11/04)
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- Preparation and application of near-infrared fluorescence probe (by machine translation)
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The invention belongs to the field of fluorescence analysis and biological micromolecule detection, and discloses a preparation method and application of a near-infrared fluorescence probe for detecting cysteine. The near-infrared fluorescence probe CN is
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Paragraph 0055-0059
(2020/07/06)
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- Symmetry-based ligand design and evaluation of small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 interaction
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The development of small molecule inhibitors of PD-1/PD-L1 is eagerly anticipated for treatment of cancer. We focused on the symmetry of the ternary complex structure of reported small molecule ligands and hPD-L1 homodimers, and designed partially- or fully-symmetric compounds for more potent inhibitors. The design of the new compounds was guided by our hypothesis that the designed symmetric compound would induce a flip of sidechain of ATyr56 protein residue to form a new cavity. The designed compound 4 exhibited substantially increased binding affinity to hPD-L1, as well as PD-1/PD-L1 inhibitory activity in physiological conditions. Compound 4 also showed a dose-dependent increase in IFN-γ secretion levels in a mixed lymphocyte reaction assay. These results not only indicate the feasibility of targeting the PD-1/PD-L1 pathway with small molecules, but illustrate the applicability of the symmetry-based ligand design as an attractive methodology for targeting protein-protein interaction stabilizers.
- Kawashita, Seiji,Aoyagi, Koichi,Yamanaka, Hiroshi,Hantani, Rie,Naruoka, Shiori,Tanimoto, Atsuo,Hori, Yuji,Toyonaga, Yukiyo,Fukushima, Kyoko,Miyazaki, Susumu,Hantani, Yoshiji
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supporting information
p. 2464 - 2467
(2019/08/20)
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- Tetrazine-Responsive Self-immolative Linkers
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Molecules that undergo activation or modulation following the addition of benign external small-molecule chemical stimuli have numerous applications. Here, we report the highly efficient “decaging” of a variety of moieties by activation of a “self-immolative” linker, by application of water-soluble and stable tetrazine, including the controlled delivery of doxorubicin in a cellular context.
- Neumann, Kevin,Jain, Sarthak,Gambardella, Alessia,Walker, Sarah E.,Valero, Elsa,Lilienkampf, Annamaria,Bradley, Mark
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- TETRAZINE AS A TRIGGER TO RELEASE CAGED CARGO
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There is presented a kit comprising a masked active agent and a tetrazine trigger, the masked active agent comprising an active agent connected to a masking moiety comprising a monovinyl ether or an active agent enclosed within a cage moiety comprising a monovinyl ether or an allyl group, wherein the tetrazine trigger is configured to release the active agent from the masking moiety or the cage moiety. Methods of preparing the masked active agents, and uses of the kit are also presented.
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Page/Page column 50-51
(2017/04/11)
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- Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors
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In order to identify potential calpain and cathepsin inhibitors we prepared 12 dihydroxychalcone analogues and tested their ability to inhibit μ-calpain, m-calpain, cathepsins B and L. In the calpain inhibition test, compound 10 exhibited the most active
- Baek, Kyung Hye,Karki, Radha,Lee, Eung-Seok,Na, Younghwa,Kwon, Youngjoo
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- Highly enantioselective synthesis of chiral 7-ring O- and N-heterocycles by a one-pot nitro-Michael-cyclization tandem reaction
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A concise enantioselective approach to synthesise medium-sized 7-ring O- and N-heterocycles has been developed. The synthetic strategy relies on an organocatalytic nitro-Michael-nitrile oxide cycloaddition tandem reaction, leading to the corresponding chiral benzoxe- and benzazepine derivatives containing an additional fused dihydroisoxazoline ring in good yields and excellent enantioselectivities (up to 97% ee).
- Rohlmann, Renate,Daniliuc, Constantin-Gabriel,Mancheno, Olga Garcia
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supporting information
p. 11665 - 11667
(2013/12/04)
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- Towards a library of chromene cannabinoids: A combinatorial approach on solid supports
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A novel solid-phase synthesis towards classical cannabinoids is presented. Starting from immobilized salicylaldehydes the desired THC-analogous tricycles are obtained in four atom-economic steps including cleavage. The reagents of the employed reactions (domino oxa-Michael-aldol, Wittig, and Diels-Alder) can be varied easily, providing the basis for a combinatorial approach. Overall yields range from 20-60%. Georg Thieme Verlag Stuttgart New York.
- Kapeller, Dagmar C.,Br?se, Stefan
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supporting information; experimental part
p. 161 - 164
(2011/03/19)
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- BORON-CONTAINING SMALL MOLECULES
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This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.
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Page/Page column 116
(2012/06/05)
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- Mechanism-based molecular design of highly selective fluorescence probes for nitrative stress
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Nitrative stress is implicated in various pathogenic processes, including neurodegenerative disorders, but there is no practical fluorescence probe which can monitor the generation of nitrative stress with high selectivity. To design a suitable fluorescence probe, we have first focused on the fluorescence quenching mechanism of the nitro group, which has been believed to be a unique quencher of fluorescent dyes. We found that nitro group-based fluorescence quenching could be explained in terms of an electron transfer process, from the excited fluorophore to the electron-deficient aromatic nitro moiety. By utilizing this result, we succeeded in developing novel fluorogenic probes, NiSPYs, which can selectively monitor the generation of nitrative stress based on aromatic nitration. NiSPYs showed strong fluorescence enhancement upon the reaction with nitrating agents, including peroxynitrite, but showed little or no fluorescence augmentation in the presence of other reactive oxygen species. NiSPYs should be potentially useful as tools to study the role of nitrative stress in various biological applications. Copyright
- Ueno, Tasuku,Urano, Yasuteru,Kojima, Hirotatsu,Nagano, Tetsuo
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p. 10640 - 10641
(2007/10/03)
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- Potent CYP19 (aromatase) 1-(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: Synthesis and biological evaluation
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The synthesis of a series of novel 1-[(benzofuran-2-yl)phenylmethyl]- pyridine, -imidazole, and -triazole derivatives is described. All the compounds were evaluated in vitro for inhibitory activity against aromatase (P450 AROM, CYP19), using hu
- Saberi, Mohammed Reza,Vinh, Tai Ky,Yee, Sook Wah,Griffiths, B. J. Nathan,Evans, Peter J.,Simons, Claire
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p. 1016 - 1022
(2007/10/03)
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- Biologically active 1,3-bis-aromatic-prop-2-en-1-ones, 1,3-bis-aromatic-propan-1-ones, and 1,3-bis-aromatic-prop-2-yn-1-ones
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The invention relates to the use of 1,3-bis-aromatic-prop-2-en-1-ones (chalcones), 1,3-bis-aromatic-propan-1-ones (dihydrochalcones), and 1,3-bis-aromatic-prop-2-yn-1-ones for the preparation of pharmaceutical compositions for the treatment or prophylaxis of a number of serious diseases including i) conditions relating to harmful effects of inflammatory cytokines, ii) conditions involving infection by Helicobacter species, iii) conditions involving infection by viruses, iv) neoplastic disorders, and v) conditions caused by microorganisms or parasites. The invention also relates to novel chalcones and dihydrochalcones (especially alkoxy substituted variants) having advantageous substitution patterns with respect to their effect as drug substances, and to methods of preparing them, as well as to pharmaceutical compositions comprising the novel chalcones. Moreover, the present invention relates to a method for the isolation of Leishmania fumarate reductase, QSAR methodologies for selecting potent compounds for the above-mentioned purposes.
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- Natural product-like combinatorial libraries based on privileged structures. 1. General principles and solid-phase synthesis of benzopyrans
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Herein we report a novel strategy for the design and construction of natural and natural product-like libraries based on the principle of privileged structures, a term originally introduced to describe structural motifs capable of interacting with a variety of unrelated molecular targets. The identification of such privileged structures in natural products is discussed, and subsequently the 2,2-dimethylbenzopyran moiety is selected as an inaugural template for the construction of natural product-like libraries via this strategy. Initially, a novel solid-phase synthesis of the benzopyran motif is developed employing a unique cycloloading strategy that relies on the use of a new, polystyrene-based selenenyl bromide resin. Once the loading, elaboration, and cleavage of these benzopyrans was established, this new solid-phase method was then thoroughly validated through the construction of six focused combinatorial libraries designed around natural and designed molecules of recent biological interest.
- Nicolaou,Pfefferkorn,Roecker,Cao,Barluenga,Mitchell
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p. 9939 - 9953
(2007/10/03)
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- Synthesis and activity of cephalosporins containing an oxyiminomethylene functionality in the ortho-position of a phenyl- or phenoxyacetic acid C-7 side chain substituent
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A new series of cephalosporins having in the C-7 side chain a phenyl- or a phenoxyacetamido group bearing an oxyiminomethyl function in the ortho-position of the aromatic ring was prepared. Their in vitro activity was tested against both Gram+ and Gram- s
- Albanese, Domenico,Landini, Dario,Leone, Mario,Penso, Michele,Zenoni, Maurizio
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p. 709 - 717
(2007/10/03)
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