95902-10-6Relevant articles and documents
Substituted dienes prepared from betulinic acid – Synthesis, cytotoxicity, mechanism of action, and pharmacological parameters
Frydrych, Ivo,Urban, Milan,?arek, Jan,Benická, Sandra,D?ubák, Petr,Gurská, Soňa,Hajdúch, Marián,Kotulová, Jana,Li?ková, Barbora,Olejníková, Denisa,Pokorny, Jan
, (2021/07/28)
A set of new substituted dienes were synthesized from betulinic acid by its oxidation to 30-oxobetulinic acid followed by the Wittig reaction. Cytotoxicity of all compounds was tested in vitro in eight cancer cell lines and two noncancer fibroblasts. Almost all dienes were more cytotoxic than betulinic acid. Compounds 4.22, 4.30, 4.33, 4.39 had IC50 below 5 μmol/L; 4.22 and 4.39 were selected for studies of the mechanism of action. Cell cycle analysis revealed an increase in the number of apoptotic cells at 5 × IC50 concentration, where activation of irreversible changes leading to cell death can be expected. Both 4.22 and 4.39 led to the accumulation of cells in the G0/G1 phase with partial inhibition of DNA/RNA synthesis at 1 × IC50 and almost complete inhibition at 5 × IC50. Interestingly, compound 4.39 at 5 × IC50 caused the accumulation of cells in the S phase. Higher concentrations of tested drugs probably inhibit more off-targets than lower concentrations. Mechanisms disrupting cellular metabolism can induce the accumulation of cells in the S phase. Both compounds 4.22 and 4.39 trigger selective apoptosis in cancer cells via intrinsic pathway, which we have demonstrated by changes in the expression of the crucial apoptosis-related protein. Pharmacological parameters of derivative 4.22 were superior to 4.39, therefore 4.22 was the finally selected candidate for the development of anticancer drug.
NEW COMPOUNDS SUITABLE AS CATALYSTS FOR POLYMERIZATION REACTIONS
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Page/Page column 54;55, (2019/04/10)
The invention relates to a compound of formula (I) and a process for synthesizing said compound. The invention further relates to the use of said compound as a catalyst, preferably for polymerization, such as, olefin polymerization. The invention also relates to the polymers produced using said catalyst and articles comprising said polymers.
A chrysene-based liquid crystalline semiconductor for organic thin-film transistors
He, Yaowu,Xu, Wenjun,Murtaza, Imran,Yao, Chao,Zhu, Yanan,Li, Aiyuan,He, Chao,Meng, Hong
, p. 3683 - 3689 (2018/04/12)
We report the synthesis and characterization of a non-liquid crystalline material, 2-phenylchrysene (Ph-CHR), and a liquid crystalline material, 2-(4-dodecyl phenyl)chrysene (C12-Ph-CHR), and discuss their organic thin-film transistor (OTFT) device perfor
Cyanostilbene deriv., light-emitting element, the light emitting device, lighting device and electronic device
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Paragraph 0457; 0458; 0459; 0460; 0461, (2019/05/01)
PROBLEM TO BE SOLVED: To provide such a novel stilbene derivative which permits the luminescence of a shorter wavelength, as is useful for a light-emitting element of a high luminous efficiency, a light-emitting device having an excellent color reproducibility and having an electric power consumption decreased, or the like. SOLUTION: This stilbene derivative is expressed by formula G11 (in the formula, with regard to R10through R12, at least one of them is a tert-butyl group, and the remainder is a hydrogen atom; with regard to R13through R15, at least one of them is a tert-butyl group, and the remainder is a hydrogen atom; and Ar4to Ar5are each a (6-25)C aryl group). COPYRIGHT: (C)2013,JPOandINPIT
Synthesis of precursors for large-diameter hemispherical buckybowls and precursors for short carbon nanotubes
Mueller, Andreas,Amsharov, Konstantin Yu.
, p. 6155 - 6164,10 (2020/09/16)
We report herein the synthesis of six precursor molecules for the rational synthesis of isomerically pure armchair, zigzag, or chiral single-walled carbon nanotubes (SWCNTs). The polycyclic aromatic hydrocarbons possess the required carbon connectivity for the generation of extended hemispherical buckybowls with predefined geometry through intramolecular cyclodehydrogenation. The precursors for the short carbon nanotubes and the large-diameter hemispherical buckybowls have potential for the rational initiation of single-chirality SWCNT growth on metal surfaces. The options for the construction of precursors for various SWCNT chiralities based on the suggested synthesis strategy are presented.
New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: Exploring the S2′ region
Malamas, Michael S.,Erdei, Jim,Gunawan, Iwan,Barnes, Keith,Hui, Yu,Johnson, Matthew,Robichaud, Albert,Zhou, Ping,Yan, Yinfa,Solvibile, William,Turner, Jim,Fan, Kristi Yi,Chopra, Rajiv,Bard, Jonathan,Pangalos, Menelas N.
body text, p. 5164 - 5170 (2011/10/09)
The proteolytic enzyme β-secretase (BACE1) plays a central role in the synthesis of the pathogenic β-amyloid in Alzheimer's disease. SAR studies of the S2′ region of the BACE1 ligand binding pocket with pyrazolyl and thienyl P2′ side chains are reported. These analogs exhibit low nanomolar potency for BACE1, and demonstrate >50- to 100-fold selectivity for the structurally related aspartyl proteases BACE2 and cathepsin D. Small groups attached at the nitrogen of the P2′ pyrazolyl moiety, together with the P3 pyrimidine nucleus projecting into the S3 region of the binding pocket, are critical components to ligand's potency and selectivity. P2′ thiophene side chain analogs are highly potent BACE1 inhibitors with excellent selectivity against cathepsin D, but only modest selectivity against BACE2. The cell-based activity of these new analogs tracked well with their increased molecular binding with EC50 values of 0.07-0.2 μM in the ELISA assay for the most potent analogs.
Configurational isomers of a stilbene-linked bis(porphyrin) tweezer: Synthesis and fullerene-binding studies
Fathalla, Maher,Jayawickramarajah, Janarthanan
supporting information; experimental part, p. 6095 - 6099 (2010/03/24)
A new stilbene-tethered bis(porphyrin) tweezer 5 has been synthesized through a Sonogashira cross-coupling reaction. The tweezer exists as two configurational isomers [(Z) + (E)], which have distinct: cavity sizes. Fullerene-binding studies show that the
Dual Pharmacophores - PDE4-Muscarinic Antagonistics
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Page/Page column 69, (2009/08/18)
The present invention is directed to novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use as dual chromaphores having inhibitory activity against PDE4 and muscarinic acetylcholine receptors (mAChRs), and thus being useful for treating respiratory diseases.
Dual Pharmacophores - PDE4-Muscarinic Antagonistics
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Page/Page column 72, (2009/08/18)
The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
Dual Pharmacophores - PDE4-Muscarinic Antagonistics
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Page/Page column 103, (2009/08/16)
The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
