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151874

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Jinyun Dong et al.
Bioorganic & medicinal chemistry, 22(24), 6876-6884 (2014-12-04)
Bcr-Abl plays an essential role in the pathogenesis and development of chronic myeloid leukaemia (CML). Inhibition of Bcr-Abl has great potential for therapeutic intervention in CML. In order to obtain novel and potent Bcr-Abl inhibitors, twenty seven 4,6-disubstituted pyrimidines were...
Amir Mahboubi et al.
Plant physiology, 168(2), 478-489 (2015-05-02)
Wood of trees is formed from carbon assimilated in the photosynthetic tissues. Determining the temporal dynamics of carbon assimilation, subsequent transport into developing wood, and incorporation to cell walls would further our understanding of wood formation in particular and tree...
Daishun Ling et al.
ACS nano, 8(8), 8027-8039 (2014-08-06)
Hepatocellular carcinoma (HCC) has one of the worst prognoses for survival as it is poorly responsive to both conventional chemotherapy and mechanism-directed therapy. This results from a lack of therapeutic concentration in the tumor tissue coupled with the highly toxic...
Benjamin J Pages et al.
Dalton transactions (Cambridge, England : 2003), 43(41), 15566-15575 (2014-09-10)
Eight platinum(II) complexes with anticancer potential have been synthesised and characterised. These complexes are of the type [Pt(I(L))(A(L))](2+), where I(L) is either dipyrido[3,2-f:2',3'-h]quinoxaline (dpq) or 2,3-dimethyl-dpq (23Me2dpq) and A(L) is one of the R,R or S,S isomers of either 1,2-diaminocyclohexane...
Iwona Kowalska et al.
Journal of agricultural and food chemistry, 62(46), 11200-11208 (2014-10-31)
Fourteen phenolic compounds (flavonoids and phenolic acids) were isolated and 19 were identified in the aerial parts of Triticum aestivum L. The structures of these compounds were established on the basis of the data obtained by electrospray ionization-mass spectrometry (ESI-MS)...
Kuruva Chandra Sekhar et al.
Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 22, 76-76 (2014-12-30)
Chronic and oral administration of benzylamine improves glucose tolerance. Picolylamine is a selective functional antagonist of the human adenosine A2B receptor. Phosphonic diamide derivatives enhance the cellular permeability and in turn their biological activities. A series of heteroaryl phosphonicdiamide derivatives...
Xinzhou Yang et al.
Journal of ethnopharmacology, 171, 161-170 (2015-06-09)
Bitter and cold Chinese medicines have been long used for the treatment for diabetes mellitus (DM) for thousands of years in China. The roots of Sophora flavescens Ait., one of bitter and cold Chinese medicines commonly used to remove lung...
Vincenzo Taresco et al.
The journal of physical chemistry. B, 119(26), 8369-8379 (2015-06-16)
Amphiphilic polyelectrolytes (APEs), exhibiting particular self-association properties in aqueous media, can be used in different industrial applications, including drug delivery systems. Their typical core-shell structure (micelle) depends on the balance of interactions between hydrophobic and ionizable monomer units. In this...
Xiu-Mei Li et al.
European journal of medicinal chemistry, 96, 436-444 (2015-04-29)
Hypericum ascyron L. has been used as a traditional medicine for the treatment of wounds, swelling, headache, nausea and abscesses in China for thousands of years. However, modern pharmacological studies are still necessary to provide a scientific basis to substantiate...
Jee Hee Suh et al.
Chemical & pharmaceutical bulletin, 63(8), 573-578 (2015-06-05)
We describe the synthesis and biological evaluation of N-aryl-5-aryloxazol-2-amine derivatives that are able to inhibit 5-lipoxygenase (5-LOX), a key enzyme of leukotriene synthesis, for the treatment of inflammation-related diseases including asthma and rheumatoid arthritis. A novel structural moiety containing oxazole...
Hannu Elo et al.
European journal of medicinal chemistry, 92, 750-753 (2015-01-27)
Certain substituted salicylaldehydes are potent antibacterial and antifungal agents and some of them merit consideration as potential chemotherapeutic agents against Candida infections, but their mechanism of action has remained obscure. We report here a distinct correlation between broadening of the...
Wieland Peschel et al.
Talanta, 140, 150-165 (2015-06-07)
The medicinal use of different chemovars and extracts of Cannabis sativa L. requires standardization beyond ∆9-tetrahydrocannabinol (THC) with complementing methods. We investigated the suitability of (1)H NMR key signals for distinction of four chemotypes measured in deuterated dimethylsulfoxide together with...
Chung Ying Chan et al.
Dalton transactions (Cambridge, England : 2003), 44(44), 19126-19140 (2015-10-20)
A series of eight Rhenium(I)-N-heterocyclic carbene (NHC) complexes of the general form [ReCl(CO)3(C^C)] (where C^C is a bis(NHC) bidentate ligand), [ReCl(CO)3(C^C)]2 (where C^C is a bis-bidentate tetra-NHC ligand) and [Re(CO)3(C^N^C)](+)[X](-) (where C^N^C is a bis(NHC)-amine ligand and the counter ion...
Rong Zhang et al.
Journal of agricultural and food chemistry, 62(33), 8302-8307 (2014-07-30)
Nonvolatile compounds play important roles in the quality of alcoholic beverages. In our previous work, a type of cyclooctapeptide lichenysin was newly identified in Chinese strong-aroma type liquor. In this work, it was found that lichenysin could selectively affect aroma...
Krzysztof Lodarski et al.
Journal of enzyme inhibition and medicinal chemistry, 30(1), 98-106 (2014-03-29)
The study presents the discovery of novel butyrylcholinesterase (BuChE) inhibitors among derivatives of azaphenothiazines by application of in silico and in vitro screening methods. From an in-house library of compounds, 143 heterocyclic molecules derived from the azaphenothiazine scaffold were chosen...
Xu-Dong Wang et al.
Bioorganic & medicinal chemistry, 23(15), 4860-4865 (2015-06-07)
3-Arylfuran-2(5H)-one derivatives show good antibacterial activity and were determined as tyrosyl-tRNA synthetase (TyrRS) inhibitors. In a systematic medicinal chemistry exploration, we demonstrated chemical opportunities to treat infections caused by Helicobacter pylori. Twenty 3-arylfuran-2(5H)-ones were synthesized and evaluated for anti-H. pylori...
Mashooq A Bhat et al.
Molecules (Basel, Switzerland), 20(10), 18246-18263 (2015-10-13)
Lead derivatives of 2-cyclohexyl-N-[(Z)-(3-methoxyphenyl/3-hydroxyphenyl) methylidene]hydrazinecarbothioamides 1-18 were synthesized, characterized and evaluated in vitro against HER-2 overexpressed breast cancer cell line SKBr-3. All the compounds showed activity against HER-2 overexpressed SKBr-3 cells with IC50 = 17.44 ± 0.01 µM to 53.29...
Zongwang Ma et al.
Applied biochemistry and biotechnology, 177(7), 1520-1529 (2015-09-17)
Bacillus mojavensis B0621A was isolated from the mantle of a pearl oyster Pinctada martensii collected from South China Sea. Semi-purified surfactins (225 mg L(-1)) were obtained by acid precipitation and vacuum flash chromatography. The component of the semi-purified surfactins was preliminarily analyzed...
Jun Zhang et al.
Sensors (Basel, Switzerland), 14(12), 24146-24155 (2014-12-18)
A new fluorescent probe P derived from naphthalimide bearing a pyridine group has been synthesized and characterized. The proposed probe P shows high selectivity and sensitivity to Cu2+ in aqueous media. Under optimized conditions, the linear response of P (2...
Julie Rakel Mikell et al.
Chemical & pharmaceutical bulletin, 63(8), 579-583 (2015-08-04)
6-Hydroxyflavanone (1) when fermented with fungal culture Cunninghamella blakesleeana (ATCC 8688a) yielded flavanone 6-O-β-D-glucopyranoside (2), flavanone 6-sulfate (3), and 6-hydroxyflavanone 7-sulfate (4). Aspergillus alliaceus (ATCC 10060) also transformed 1 to metabolite 3 as well as 4'-hydroxyflavanone 6-sulfate (5) and 6,4'-dihydroxyflavanone...
Xuejiao Liu et al.
Journal of drug targeting, 23(5), 417-426 (2015-02-07)
Hypericin is a necrosis avid agent useful for nuclear imaging and tumor therapy. Protohypericin, with a similar structure to hypericin except poorer planarity, is the precursor of hypericin. In this study, we aimed to investigate the impact of this structural...
Synthesis of 6-(2-hydroxybenzoyl) pyrazolo [1, 5-a] pyrimidines by reaction of 5-amino-1h-pyrazoles and 3-formylchromone
Quiroga J, et al.
Journal of Heterocyclic Chemistry, 39(1), 51-54 (2002)
Ahmed M Younis et al.
International journal of medicinal mushrooms, 17(6), 579-590 (2015-09-10)
Pleurotus ostreatus is an edible mushroom that also has high medicinal values. In this study, P. ostreatus was tested for its ability to inhibit the growth of fungi and bacteria. The freeze-dried fruiting body, broth from submerged culture, and mycelial...
Yingli Yang et al.
Oncology reports, 34(3), 1311-1318 (2015-07-03)
In the present study, 2-pyridinecarboxaldehyde 2-pyridinecarboxylic acid hydrazone (PPAH) was prepared and its antitumor activity was evaluated. The inhibition of proliferation of PPAH against the HepG2 and HCT-116 cell lines was less effective, yet in the presence of copper ions...
Denis A Babkov et al.
Bioorganic & medicinal chemistry, 23(21), 7035-7044 (2015-10-08)
The need for novel therapeutic options to fight herpesvirus infections still persists. Herein we report the design, synthesis and antiviral evaluation of a new family of non-nucleoside antivirals, derived from 1-[ω-(4-bromophenoxy)alkyl]uracil derivatives--previously reported inhibitors of human cytomegalovirus (HCMV). Introduction of...
Yan Tan et al.
Biomaterials, 56, 219-228 (2015-05-03)
Serious challenges remain in immunotherapy, such as to effectively deliver antigens and non-invasively monitor biological processes. Therefore, we aim to design a useful nanocarrier for enhancing antigen-specific immune response and performing functional molecular imaging guided immunotherapy. To achieve this goal...
Navneet Chandak et al.
Journal of enzyme inhibition and medicinal chemistry, 29(4), 476-484 (2013-06-20)
Synthesis of total eighteen 2-amino-substituted 4-coumarinylthiazoles including sixteen new compounds (3a-o and 5b) bearing the benzenesulfonamide moiety is described in the present report. All the synthesized target compounds were examined for their in vivo anti-inflammatory (AI) activity and in vitro...
Nirmalya Bandyopadhyay et al.
European journal of medicinal chemistry, 89, 59-66 (2014-12-03)
The title monomeric Pd(II) compound, [Pd(L)(Cl)], was synthesized in moderate yield out of the reaction of equimolar proportion of Na2[PdCl4] and 3-[(5-bromo-2-hydroxy-benzylidene)-hydrazono]-butan-2-one oxime (LH) in tetrahydrofuran milieu. LH is a 1:1 Schiff-base condensate of 2,3-butanedionemonoxime monohydrazone and 5-bromosalicylaldehyde. [Pd(L)(Cl)] has...
Nripendra Nath Biswas et al.
Organic & biomolecular chemistry, 13(3), 925-937 (2014-11-20)
Gram-negative bacteria such as Pseudomonas aeruginosa use N-acylated L-homoserine lactones (AHLs) as autoinducers (AIs) for quorum sensing (QS), a major regulatory and cell-to-cell communication system for social adaptation, virulence factor production, biofilm formation and antibiotic resistance. Some bacteria use indole...
Xuesheng Zhang et al.
Chemosphere, 134, 84-90 (2015-04-29)
In the present study, twenty-six types of polymethoxylated diphenyl ethers (PMeODEs), twenty types of polyhydroxylated diphenyl ethers (PHODEs), seven types of methoxylated-polychlorinated diphenyl ethers (MeO-PCDEs) and seven types of hydroxylated-polychlorinated diphenyl ethers (HO-PCDEs) were synthesized. The logKow and logKoc values...
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