Conducting blends of poly(diphenylamine) (PDPA) doped with H2SO4 or p-toluenesulphonic acid (TSA) and poly(vinylidene fluoride) (PVDF) were successfully prepared by using N,N′-dimethyl formamide (DMF) as solvent. Flexible, free-standing and conducting polyblends were obtained by solution castin...
In this work, poly (3-methylthiophene) (P3MT) or poly (3-octylthiophene) (P3OT) films were synthesized electrochemically with polydiphenylamine (PDFA), in layers and blended copolymers, in non-aqueous media through the oxidation of the monomers, using a standard three-electrode cell in acetonitr...
The electrochemical oxidation of the hole conducting material N,N′-diphenylbenzidine (DPB) in N,N-dimethylformamide (DMF) was investigated by cyclic voltammetry and spectroelectrochemistry. The results were compared to electro-oxidation in acetonitrile. Time-resolved UV–Vis spectroscopy, with ...
Several N-(2,2-diphenylvinyl)-N,N′-diphenylbenzidine-based derivatives were synthesized by the multi-step synthetic route. Full characterization of their structure is presented. The synthesized materials were examined by various techniques including differential scanning calorimetry, UV spectro...
Combretastatin A-4 phosphate (CA4P) selectively blocks tumor blood flow. However, the detailed mechanisms through which CA4P specifically affects tumor blood vessels are not well understood. Recent reports revealed that tumor tissue-derived endothelial cells (TECs) have various specific features...
We here describe the preparation of a series of hybrid molecules containing a combretastatin A-4 moiety and a pironetin analogue fragment connected through a spacer of variable length which includes a 1,2,3-triazole ring. The cytotoxic activities of these compounds have been measured. Relations ...
Glucuronidation by uridine 5-diphosphoglucuronosyl transferase enzymes (UGTs) is a cause of intrinsic drug resistance in cancer cells. Glucuronidation of combretastatin A-4 (CA-4) was previously identified as a mechanism of resistance in hepatocellular cancer cells. Herein, we propose chemical m...
A series of colchicine site binding tubulin inhibitors were designed and synthesized by the modification of the combretastatin A-4 (CA4) pharmacophore. The ring B was replaced by the pharmacologically relevant benzimidazole or benzothiazole scaffolds, and the cis-configuration of the olefinic bo...
In order to design and synthesize a new class of heterocyclic analogues of natural combretastatin A-4 and its synthetic derivative AVE8062, the benzoxazolone ring was selected as a scaffold for a bioisosteric replacement of the ring B of both molecules. A library of 28 cis- and trans-styrylbenzo...
A series of pyrrole analogues of combretastatin (CA-4) were synthesized and tested for their anti-proliferative activity. The highly diastereoselective acyl-Claisen rearrangement was used to provide 2,3-syn disubstituted morpholine amides which were used as precursors for the various analogues. ...
Combretastatin A-4 phosphate (CA4P) induces tumor necrosis by selectively inhibiting tumor blood flow. However, the detailed mechanisms by which CA4P selectively disrupts tumor blood vessels are not well understood. Our previous study indicated that the selective blocking effect of CA4P might be...
The worldwide prevalence of NDM-1-producing bacteria has drastically undermined the clinical efficacy of the last line antibiotic of carbapenems, prompting a need to devise effective strategy to preserve their clinical value. Our previous studies have shown that ebselen can restore the efficacy ...
The total synthesis of two isoflavone C-glycosides (6-tert-butylpuerarin and 6-tert-butyl-4′-methoxypuerarin) was achieved through the deoxybenzoin pathway with overall yields of 14.6% and 14.2%. The key intermediate 12 was obtained by de-tert-butylation of 10 with trifluoroacetic acid and Frie...
A rapid, sensitive and specific ultra performance liquid chromatography-tandem mass spectrometry (UPLC–MS/MS) method for the quantification of shanzhiside methyl ester, 8-O-acetylshanzhiside methyl ester and luteolin-7-O-β-d-glucopyranoside of Lamiophlomis rotata Pill in rat plasma was develop...
A number of 2-hydroxy-6-methyl-7-(arylamino)-1,7-dihydropurin-8-ones have been synthesized. 3-Oxo-2-(arylhydrazono)butyric acid ethyl ester were acetylated and treated with triethyl amine and formamide in presence of 1,4-dioxane to yield N-(5-acetyl-4-ethoxy-2-oxo-2,5-dihydro-imidazol-1-yl)-N-ar...
A novel 7-hydroxy-4-methyl-8-(p-tolylazo)-2H-1-benzopyran-2-one (coumarin) (L1) and 7-hydroxy-4-methyl-8-(p-anisylazo)-2H-1-benzopyran-2-one (coumarin) (L2) and their metal complexes with Mn(II), Co(II), Ni(II) Cu(II) and Zn(II) have been prepared and characterized by elemental analysis, infrare...
A toxicologic and dermatologic review of 1-[5(Or 6)-Methyl-7(or 8)-1-(methylethyl)bicyclo[2.2.2]oct-5-en-2-yl]ethan-1-one when used as a fragrance ingredient is presented. 1-[5(Or 6)-Methyl-7(or 8)-1-(methylethyl)bicyclo[2.2.2]oct-5-en-2-yl]ethan-1-one is a member of the fragrance structural gro...
Based on a previous report that a series of 8-(phenoxymethyl)-xanthines may be promising leads for the design of A1 adenosine receptor antagonists, selected novel and known 1,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine and 1,3,7-trimethyl-8-(phenoxymethyl)-xanthine analogs were synthesized and...
A simple, robust and efficient Rh(III)-catalyzed synthesis of novel 12H-indazolo[2,1-a]cinnolin-12-ones has been developed via tandem C–H activation/annulation of 2-phenylindazolones with diazo compounds by using less developed secondary amine as an intrinsic directing group. Notably, a series ...
[1,2,3]Triazolo[4,5-h][1,6]naphthyridines and [1,3]oxazolo[5,4-h][1,6]naphthyridines were synthesized with the aim to investigate their photocytotoxic activity. Upon irradiation, oxazolo-naphtapyridines induced light-dependent cell death at nanomolar/low micromolar concentrations (EC50 0.01–6.5...
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