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Kylie A MacGregor et al.
European journal of medicinal chemistry, 85, 191-206 (2014-08-02)
Virtual screening of the ChemDiversity and ChemBridge compound databases against dynamin I (dynI) GTPase activity identified 2,5-bis-(benzylamino)-1,4-benzoquinone 1 as a 273 ± 106 μM inhibitor. In silico lead optimization and focused library-led synthesis resulted in the development of four discrete benzoquinone/naphthoquinone based compound
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
Yunbin Xiao et al.
International journal of nanomedicine, 10, 1155-1172 (2015-02-25)
Magnetic resonance imaging (MRI) contrast agents based on chitosan derivatives have great potential for diagnosing diseases. However, stable tumor-targeted MRI contrast agents using micelles prepared from high molecular weight chitosan derivatives are seldom reported. In this study, we developed a
Yuanyuan Wu et al.
Journal of fluorescence, 25(4), 961-972 (2015-05-20)
4-N,N'-dimethylamino-4'-N'-stilbenemaleamic acid (DASMA), a unique molecular photochrome probe that exhibits solubility and retains trans-cis photoisomerisation in a wide range of organic solvents and aqueous pH environments, was prepared, purified and chemically characterised. Absorption, fluorescence excitation and emission spectra and constant-illumination
Amer M Alanazi et al.
European journal of medicinal chemistry, 92, 115-123 (2015-01-01)
A group of 30 cyclic imides (1-10a-c) was designed for evaluation as a selective COX-2 inhibitor and investigated in vivo for anti-inflammatory and analgesic activities. Compounds 6a, 6b, 7a and 7b exhibit optimal COX-2 inhibitory potency (IC50 = 0.18, 0.24, 0.28 and 0.36 μM;
Amreddy Narsireddy et al.
International journal of nanomedicine, 10, 6865-6878 (2015-11-26)
Challenges in photodynamic therapy (PDT) include development of efficient near infrared-sensitive photosensitizers (5,10,15,20-tetrakis(4-hydroxyphenyl)-21H,23H-porphine [PS]) and targeted delivery of PS to the tumor tissue. In this study, a dual functional dendrimer was synthesized for targeted PDT. For targeting, a poly(amidoamine) dendrimer
Kun-Ming Jiang et al.
Medicinal chemistry (Shariqah (United Arab Emirates)), 11(5), 453-461 (2014-12-30)
A new series of (E)-N,2,3-triarylacrylamide derivatives were designed and synthesized as potent anticancer agents. Cytotoxicity of the 26 target compounds was evaluated in vitro against six cancer cell lines (HCT116, A549, MDA-MB-468, HepG2, SKNMC and SK-OV-3) by Sulforhodamine B colorimetric
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
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
Tristan Gollnest et al.
Nature communications, 6, 8716-8716 (2015-10-28)
The antiviral activity of nucleoside reverse transcriptase inhibitors is often limited by ineffective phosphorylation. We report on a nucleoside triphosphate (NTP) prodrug approach in which the γ-phosphate of NTPs is bioreversibly modified. A series of TriPPPro-compounds bearing two lipophilic masking
Zhigang Nie et al.
Molecular medicine reports, 20(1), 401-408 (2019-05-23)
Osteoblast apoptosis has been identified as an important event in the development of glucocorticoid (GC)‑induced osteoporosis and osteonecrosis of the femoral head. Crocin, a bioactive ingredient of saffron, has been demonstrated to induce antiapoptotic effects on numerous types of cell in vitro;
Yasemin Sahbaz et al.
Molecular pharmaceutics, 12(6), 1980-1991 (2015-04-24)
Absorption after oral administration is a requirement for almost all drug products but is a challenge for drugs with intrinsically low water solubility. Here, the weakly basic, poorly water-soluble drugs (PWSDs) itraconazole, cinnarizine, and halofantrine were converted into lipophilic ionic
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
Ting-Ting You et al.
Bioresource technology, 199, 271-274 (2015-09-14)
Acid enhanced ionic liquid (IL) 1-n-butyl-3-methylimidazolium chloride ([C4 mim]Cl) pretreatment has shown great potential for boosting the yield of sugars from biomass cost-effectively and environmental-friendly. Pretreatment with shorter processing time will promote the commercial viability. In this work, pretreatment of
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
Virsinha Reddy et al.
Organic & biomolecular chemistry, 13(12), 3732-3741 (2015-02-18)
An efficient and mild protocol for the direct construction of aryl- and alkyl-substituted isoquinolines has been realized through silver nitrate catalyzed aromatic annulation of o-(1-alkynyl)arylaldehydes and ketones with ammonium acetate. The salient feature of this methodology is that this annulation
Phuong Hoang Tran et al.
Molecules (Basel, Switzerland), 20(10), 19605-19619 (2015-10-31)
A fast and green method is developed for regioselective acylation of indoles in the 3-position without the need for protection of the NH position. The method is based on Friedel-Crafts acylation using acid anhydrides. The method has been optimized, and
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
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
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
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
A Nikolova et al.
Drug research, 65(6), 317-322 (2014-07-06)
In this work we present 3 new complexes of Ruthenium (III) with a general formula HL[Ru(L)2Cl4], where L=benzothiazole, 2-methylbenzothiazole and 2-mercaptobenzothiazole. The syntheses were carried out in polar medium under argon. The compounds obtained were characterised by IR-, (1)H-NMR- (13)C-NMR-
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
Xiaofei Chen et al.
Biomaterials science, 3(6), 870-878 (2015-07-30)
Herein, hyperbranched poly(ethylene glycol)-based supramolecular nanoparticles with pH-sensitive properties were designed and used for targeted drug delivery. Via host-guest recognition between benzimidazole anchored poly(ethylene glycol)-hyperbranched polyglycerol (PEG-HPG-BM) and folic acid modified CD (FA-CD), targeted supramolecular nanoparticles (TSNs) were fabricated. At
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
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
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
Vladimir E Oslovsky et al.
Nucleosides, nucleotides & nucleic acids, 34(7), 475-499 (2015-07-15)
Several methods for the preparation of some N(6)-substituted adenosines based on selective 1-N-alkylation with subsequent Dimroth rearrangement were developed. The proposed methods seem to be effective for the preparation of natural N(6)-isopentenyl- and N(6)-benzyladenosines, which are known to possess pronounced
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
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