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关键词:'piperidones'
显示 31-60 共 254 条结果 关于 "piperidones" 范围 论文
B G Choi et al.
Archives of pharmacal research, 21(2), 157-163 (1999-01-06)
Several aniline mustard analogues were obtained by introducing N,N-bis(2-chloroethyl)amino moiety to phenyl ring of A10 analogues in order to increase reactivity of A10 analogs and selectivity into DNA. The in vitro antitumor activity of synthesized compounds was evaluated using five
Xin Wang et al.
Molecular pharmacology, 85(6), 932-945 (2014-04-10)
b-AP15 [(3E,5E)-3,5-bis[(4-nitrophenyl)methylidene]-1-(prop-2-enoyl)piperidin-4-one] is a small molecule inhibitor of the ubiquitin specific peptidase (USP) 14/ubiquitin carboxyl-terminal hydrolase (UCH) L5 deubiquitinases of the 19S proteasome that shows antitumor activity in a number of tumor models, including multiple myeloma. b-AP15 contains an α,β-unsaturated
Manuel A P Segurado et al.
The Journal of organic chemistry, 72(14), 5327-5336 (2007-06-15)
Rate constants were measured for the oxidative chlorodehydrogenation of (R,S)-2-phenoxypropanoic acid and nine ortho-, ten para- and five meta-substituted derivatives using (R,S)-1-chloro-3-methyl-2,6-diphenylpiperidin-4-one (NCP) as chlorinating agent. The kinetics was run in 50% (v/v) aqueous acetic acid acidified with perchloric acid
Dani Youssef et al.
Bioorganic & medicinal chemistry letters, 19(22), 6364-6367 (2009-10-13)
A novel series of maleamic amino acid ester conjugates of 3,5-bisarylmethylene-4-piperidones were prepared to investigate the efficacy of micronutrient conjugation in enhancing cytotoxic potency by improving selectivity and delivery. These compounds, prepared as anticancer agents, were expected to demonstrate enhanced
Ning Li et al.
European journal of medicinal chemistry, 155, 531-544 (2018-06-18)
Ten novel symmetric 3,5-bis(arylidene)-4-piperidone derivatives (BAPs, 1-10) and fourteen dissymmetric BAPs (11-24) were synthesized and evaluated the cytotoxicity. All of the compounds have been screened for their anti-inflammatory activity characterized by evaluating their inhibitory effects on LPS-induced IL-6, TNF-α secretion.
M Agostinha R Matos et al.
The journal of physical chemistry. A, 112(40), 10053-10058 (2008-09-09)
The standard (p(o) = 0.1 MPa) molar energies of combustion in oxygen, at T = 298.15 K, of solid 3,3-tetramethyleneglutaric acid and the related 3,3-tetramethyleneglutaric anhydride and 3,3-tetramethyleneglutarimide were measured by static bomb combustion calorimetry. The values of the standard
Jianhua Ju et al.
Bioorganic & medicinal chemistry letters, 18(22), 5951-5954 (2008-08-08)
Lactimidomycin (LTM, 1), iso-migrastatin (iso-MGS, 2) and migrastatin (MGS, 3) are macrolide antitumor antibiotics differing in macrolide ring size but all bearing a glutarimide side chain. To further develop these natural products and related analogs as drug candidates we have
Wenji Yin et al.
Drug metabolism and disposition: the biological fate of chemicals, 31(2), 215-223 (2003-01-16)
We describe herein a novel metabolic fate of the 2,2,6,6-tetramethyl-piperidine (2,2,6,6-TMPi) moiety to a ring-contracted 2,2-dimethyl pyrrolidine (2,2-DMPy) in human liver microsomal incubations. The existence of this pathway was demonstrated for three compounds (I-III) of varied structures suggesting that this
Najmeh Edraki et al.
Iranian journal of pharmaceutical research : IJPR, 15(2), 425-437 (2016-09-20)
1-[4-(2-Alkylaminoethoxy) phenylcarbonyl]-3,5-bis(arylidene)-4-piperidones are a novel class of potent cytotoxic agents. These compounds demonstrate low micromolar to submicromolar IC50 values against human Molt 4/C8 and CEM T-lymphocytes and murine leukemia L1210 cells. In this study, a comparative QSAR investigation was performed
Alexander A Bisset et al.
Chemical communications (Cambridge, England), 48(98), 11978-11980 (2012-11-07)
The synthesis of (3E)-1-benzyl-3-[(2-oxopyridin-1(2H)-yl)methylidene]piperidine-2,6-dione 5 from N-benzylglutarimide was achieved in three steps. The asymmetric hydrogenation of 4 gave either the product of partial reduction (10) or full reduction (13), depending on the catalyst which was employed, in high ee in
Mercedes Amat et al.
The Journal of organic chemistry, 74(3), 1205-1211 (2008-12-17)
The enantioselective construction of the 3-ethylindolo[2,3-a]quinolizidine moiety present in numerous indole alkaloids is reported, the key steps being a stereoselective cyclocondensation of (S)-tryptophanol with an appropriate racemic delta-oxoester and a regio- and stereoselective cyclization of the resulting oxazolopiperidones on the
M Hilal Sehitoglu et al.
Journal of enzyme inhibition and medicinal chemistry, 30(2), 264-269 (2014-06-19)
In the present study, in order to evaluate antioxidant and radical scavenging properties of Pistachio gum (P-Gum), different bioanalytical methods such as DPPH(•) scavenging activity, DMPD(•+) radical scavenging activity, total antioxidant activity determination by ferric thiocyanate, reducing ability Fe(3+)-Fe(2+) transformation
T Kondo et al.
Radiation research, 127(1), 11-18 (1991-07-01)
The possible use of 2,2,6,6-tetramethyl-4-piperidone (TMPone) for the detection of singlet oxygen was investigated by gamma radiolysis and sonolysis of oxygen-saturated aqueous solutions. Formation of 2,2,6,6-tetra-methyl-4-piperidone-N-oxyl (TAN) was observed with both gamma radiolysis and sonolysis with a similar dependence on
R Konaka et al.
Redox report : communications in free radical research, 6(5), 319-325 (2002-01-10)
We previously reported that irradiation of titanium dioxide (TiO2) in ethanol generates both singlet oxygen (1O2) and superoxide anion (O2*-) as measured by EPR spectroscopy. The present study describes the production of reactive oxygen species upon irradiation of TiO2 in
Jianhua Ju et al.
Journal of the American Chemical Society, 131(4), 1370-1371 (2009-01-10)
Migrastatin (1), iso-migrastatin (5) and lactimidomycin (7) are all glutarimide-containing polyketides known for their unique structures and cytotoxic activities against human cancer cell lines. Migrastatin, a strong inhibitor of tumor cell migration, has been an important lead in the development
Oak-Kee Hong et al.
Endocrinology and metabolism (Seoul, Korea), 35(2), 384-395 (2020-07-04)
Endothelial-to-mesenchymal transition (EndMT) contributes to inflammatory conditions inducing conversion of endothelial cells (ECs) into activated fibroblasts, promoting fibrotic diseases. Pro-inflammatory cytokine is the most potent inducer of EndMT. We investigated inhibition of interleukin-1β (IL-1β)-induced EndMT by gemigliptin, a dipeptidyl peptidase-IV
Shin Nishiumi et al.
Archives of biochemistry and biophysics, 470(2), 187-199 (2007-12-19)
Halogenated and polycyclic aromatic hydrocarbons, exogenous ligands of the aryl hydrocarbon receptor (AhR), cause various toxicological effects through the transformation of the AhR. In this study, we investigated the antagonistic effects of indigoids on the transformation in addition to their
Mizuki Kuboki et al.
Biochemical and biophysical research communications, 456(3), 810-814 (2014-12-17)
DTCM-glutarimide (DTCM-G) is a newly found anti-inflammatory agent. In the course of experiments with lymphoma cells, we found that DTCM-G induced specific RelB cleavage. Anticancer agent vinblastine also induced the specific RelB cleavage in human fibrosarcoma HT1080 cells. The site-directed
Deevi Basavaiah et al.
Organic & biomolecular chemistry, 6(6), 1034-1039 (2008-03-11)
A simple and convenient synthesis of di(E)-arylidene-tetralone-spiro-glutarimides from Baylis-Hillman acetates via an interesting biscyclization strategy involving facile C-C and C-N bond formation is described. Also, one-pot multistep transformation of the Baylis-Hillman acetates into di(E)-arylidene-spiro-bisglutarimides is presented.
Mercedes Amat et al.
Chemical communications (Cambridge, England), (20)(20), 2935-2937 (2009-05-14)
The first total synthesis of (-)-16-episilicine has been completed from a phenylglycinol-derived bicyclic lactam, the key steps being stereoselective conjugate addition and alkylation reactions, and a ring-closing metathesis.
Hiroshi Tsuchikawa et al.
Organic letters, 14(9), 2326-2329 (2012-04-26)
Chiral 2-piperidinone compounds with various C-6 substituents were successfully synthesized via a Pd-catalyzed asymmetric 6-endo cyclization of dienamides, which were evidently activated by both N-p-toluenesulfonyl and C-3 ester substituents.
Pei-Qiang Huang et al.
Organic letters, 8(7), 1435-1438 (2006-03-28)
[reaction: see text] Using 5b as a common intermediate, the first asymmetric synthesis of (-)-epiquinamide (4) and a formal asymmetric synthesis of (-)-homopumiliotoxin 223G (2) is described. A key feature of our approach is the flexible introduction of a functionalized
Xiaonan Zhang et al.
Oxidative medicine and cellular longevity, 2019, 1659468-1659468 (2019-07-10)
Inhibitors of the 20S proteasome such as bortezomib are cytotoxic to tumor cells and have been proven to be valuable for the clinical management of multiple myeloma. The therapeutic efficacy of bortezomib is, however, hampered by the emergence of acquired
M V Kumari et al.
Biochemistry and molecular biology international, 38(6), 1163-1170 (1996-05-01)
"beta CATECHIN", a preparation containing green tea extract, ascorbic acid, sunflower seed extract, dunaliella carotene and natural vitamin E, has been designed as a model "universal antioxidant" that offers protection via its scavenging action on a wide range of free
Swagatika Das et al.
ChemMedChem, 6(10), 1892-1899 (2011-08-10)
The principal objective of this study was the examination of the theory of cytotoxic synergism. In this exploratory study, we tested the hypothesis that doubling the number of sites available for thiol alkylation in a series of candidate cytotoxins increases
Hideki Kubota et al.
Bioorganic & medicinal chemistry letters, 14(12), 3049-3052 (2004-05-20)
A series of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives were synthesized, and their bradycardic activities were investigated in the isolated right atria of guinea pigs and in conscious rats. These efforts identified the achiral compound 2f, which exhibited potent and long-lasting bradycardic activity with
Shyam Raj Yadav et al.
Chirality, 27(9), 619-624 (2015-06-17)
A simple and stereoselective synthesis of 3-methylthalidomide, a configurationally stable thalidomide analog, is presented. Herein we describe the synthesis of (R)-3-methylthalidomide starting from (S)-alanine by piperidin-2-one ring assembly approach in high yield and enantiomeric purity without using a chiral auxiliary
Ahmed Mahjoub et al.
Chemphyschem : a European journal of chemical physics and physical chemistry, 12(10), 1822-1832 (2011-05-28)
We studied the single-photon ionization of gas-phase δ-valerolactam (piperidin-2-one) and of its dimer using vacuum-ultraviolet (VUV) synchrotron radiation coupled to a velocity map imaging electron/ion coincidence spectrometer. The slow photoelectron spectrum (SPES) of the monomer is dominated by the vibrational
Synthesis, structures and anti-HBV activities of derivatives of the glutarimide antibiotic cycloheximide.
Hui-fang Guo et al.
The Journal of antibiotics, 62(11), 639-642 (2009-08-29)
Chuanjin Tian et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 18(45), 14305-14313 (2012-10-16)
The significance of the molecular chirality of drugs has been widely recognized due to the thalidomide tragedy. Most of the new drugs reaching the market today are single enantiomers, rather than racemic mixtures. However, many optically pure drugs, including thalidomide
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