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Guoliang Zhao - One of the best experts on this subject based on the ideXlab platform.
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synthesis crystal structure and biological activity of a nickel ii complex constructed by 2 phenyl 4 Selenazole carboxylic acid and 1 10 phenanthroline
Journal of Coordination Chemistry, 2013Co-Authors: Pei Shi, Xia Shi, Quanyin Guan, Guoliang ZhaoAbstract:A nickel(II) complex, [NiL(phen)2]L·5H2O (HL = 2-phenyl-4-Selenazole carboxylic acid, C10H7O2NSe, phen = 1,10-phenanthroline), was synthesized and characterized by elemental analysis and IR. The single crystal structure was determined by single-crystal X-ray diffraction. C88H78N12Ni2O19Se4 crystallized in the triclinic system, space group Pī. The interaction between the complex and the calf thymus DNA was studied by an ethidium bromide fluorescent probe. The antibacterial activities of the complex and ligand against five species of bacteria, Escherichia coli, Staphylococcus epidermidis, Streptococcus viridans, Staphylococcus aureus and Acinetobacter baumanii, were tested. The anticancer activities of the complex against human pancreatic cancer line PANC-28 and human hepatocarcinoma line HuH7 were also studied by employing an MTT assay.
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2 phenyl 1 3 Selenazole 4 carb oxy lic acid
Acta Crystallographica Section E-structure Reports Online, 2011Co-Authors: Jinbei Shen, Jifei Chen, Yufeng Zhou, Guoliang ZhaoAbstract:In the title compound, C10H7NO2Se, the two rings are twisted, making a dihedral angle of 12.42 (9)°. In the crystal, pairs of molecules are disposed about an inversion center, generating O—H⋯O hydrogen-bonded dimers.
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tris 1 10 phenanthroline κn n zinc ii chloride 2 phenyl 4 Selenazole 5 car box yl ate decahydrate
Acta Crystallographica Section E-structure Reports Online, 2011Co-Authors: Jinbei Shen, Jifei Chen, Yufeng Zhou, Guoliang ZhaoAbstract:The asymmetric unit of the title salt, [Zn(C12H8N2)3](C10H6NO2Se)Cl·10H2O, contains a [Zn(phen)3]2+ cation (phen is 1,10-phenanthroline), uncoordinated chloride and 2-phenyl-4-Selenazole-5-carboxylate anions and ten uncoordinated water molecules. The central ZnII ion is six-coordinated by six N atoms from three phen ligands in a distorted octahedral geometry. An extensive O—H⋯O, O—H⋯N and O—H⋯Cl hydrogen-bonding network stabilizes the crystal structure.
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Tris(1,10-phenanthroline-κ2N,N′)zinc(II) chloride 2-phenyl-4-Selenazole-5-carboxylate decahydrate
International Union of Crystallography, 2011Co-Authors: Jinbei Shen, Jifei Chen, Yufeng Zhou, Guoliang ZhaoAbstract:The asymmetric unit of the title salt, [Zn(C12H8N2)3](C10H6NO2Se)Cl·10H2O, contains a [Zn(phen)3]2+ cation (phen is 1,10-phenanthroline), uncoordinated chloride and 2-phenyl-4-Selenazole-5-carboxylate anions and ten uncoordinated water molecules. The central ZnII ion is six-coordinated by six N atoms from three phen ligands in a distorted octahedral geometry. An extensive O—H...O, O—H...N and O—H...Cl hydrogen-bonding network stabilizes the crystal structure
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synthesis crystal structures and biological activity of transition metal complexes of 2 phenyl 4 Selenazole carboxylic acid
SCIENTIA SINICA Chimica, 2010Co-Authors: Guoliang Zhao, Linxiang Shao, Huiduo Xian, Junping Zhang, Jianfeng Liu, Xia ShiAbstract:2-Phenyl-4-Selenazole carboxylic acid ( HL ) and its six transition metal complexes [ML2(H2O)2] ( M= Co, Ni, Cu, Cd) 1–4, [ZnL2](5), [CuL2(py)2](6) were synthesized and characterized by elemental analysis, IR spectra, thermal analysis. Crystal structures of complexes 3 and 6 were determined by single-crystal X-ray diffraction method. The interaction between 7 compounds and DNA were studied by EtBr fluorescent probe. The antibacterial activity of 7 compounds against six species of bacteria which are E.coli JM109, E.coli, DH5α, S. epidermidis, S. aureus, baumanii, S. viridans were tested respectively. Also the inhibition of 7 componnds against normal cell 293T and tumor cell RAW 264.7 were tested.
Leroy B Townsend - One of the best experts on this subject based on the ideXlab platform.
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synthesis of 2 4 disubstituted thiazoles and Selenazoles as potential antifilarial and antitumor agents 2 2 arylamido and 2 alkylamido derivatives of 2 amino 4 isothiocyanatomethyl thiazole and 2 amino 4 isothiocyanatomethyl Selenazole
Journal of Medicinal Chemistry, 1993Co-Authors: Y Kumar, Rachel Green, Dean S Wise, Linda L Wotring, Leroy B TownsendAbstract:The synthesis of a series of 2-arylamido and 2-alkylamido derivatives of 2-amino-4-(isothiocyanatomethyl)thiazole and 2-amino-4-(isothiocyanatomethyl)Selenazole is described. In vitro antiproliferative evaluations were carried out using L1210 cells. The 2-(alkylamido)thiazole derivatives were moderately antiproliferative, with IC50's of 4-8 microM. A significant increase in activity was obtained for the arylamido derivatives, with IC50's of 0.2-1 microM. The results obtained for the Selenazoles were similar to those for the thiazoles. 2-Benzamido-4-(isothiocyanatomethyl)-thiazole (19) was found to be a potent inhibitor of GMP synthetase. None of the compounds prepared in this study demonstrated antifilarial activity.
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synthesis of 2 4 disubstituted thiazoles and Selenazoles as potential antitumor and antifilarial agents 1 methyl 4 isothiocyanatomethyl thiazole 2 carbamates Selenazole 2 carbamates and related derivatives
Journal of Medicinal Chemistry, 1993Co-Authors: Y Kumar, Rachel Green, Dean S Wise, Linda L Wotring, Katherine Z Borysko, Leroy B TownsendAbstract:Methyl 4-(isothiocyanatomethyl)thiazole-2-carbamate and methyl 4-(isothiocyanatomethyl)Selenazole-2-carbamate have been prepared via chemical transformations involving 2-amino-4-(chloromethyl)thiazole (1) and 2-amino-4-(chloromethyl)Selenazole (2), respectively, as starting materials. The homoanalog, methyl 4-(2-isothiocyanatoethyl)thiazole-2-carbamate, was prepared from (2-aminothiazol-4-yl)acetic acid. All compounds prepared were evaluated for their ability to inhibit leukemia L1210 cell proliferation. Methyl 4-(isothiocyanatomethyl)thiazole-2-carbamate (7) was the most active compound in this screen, inhibiting the growth of L1210 leukemic cells with an IC50 = 3.2 microM. Mitotic blocking appears to be its primary mechanism of cytotoxic activity. Compound 7 also was the only compound which demonstrated significant in vivo antifilarial activity against the adult worms of Acanthocheilonema viteae in experimentally infected jirds. This compound was inactive against Brugia pahangi at a dosage of 100 mg/kg x 5 days.
Hideharu Ishihara - One of the best experts on this subject based on the ideXlab platform.
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a facile synthesis of 2 amino 1 3 Selenazole by reaction of n n unsubstituted selenourea with ketone
Heteroatom Chemistry, 2006Co-Authors: Mamoru Koketsu, Hiromune Ando, Koichi Kanoh, Hideharu IshiharaAbstract:2-Dialkylamino-1,3-Selenazoles were yielded by the reaction of N,N-unsubstituted selenoureas with ketones in the presence of ferric chloride. © 2006 Wiley Periodicals, Inc. Heteroatom Chem 17:88–92, 2006; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20180
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a facile preparation of 2 amino 1 3 Selenazoles by reactions of n n unsubstituted selenoureas with chloroacetonitrile
Chemistry Letters, 2005Co-Authors: Mamoru Koketsu, Hidenori Tanaka, Hideharu IshiharaAbstract:Reactions of N,N-unsubstituted selenoureas 1 with chloroacetonitrile 2 was investigated. When anhydrous solvent was used, the reaction gave cyanomethyl 1-piperidinoselenocarboimidate hydrochloride 3. The reaction in solvent including water yielded 2-amino-4,5-dihydro-l,3-selenazol-4-iminium chlorides 4 in moderate to high yields.
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Facile preparation of 1,3-Selenazole-5-carboxylic acids and the carboxylates by Reaction of selenazadienes with chloroacetyl chloride
Synthesis, 2004Co-Authors: Mamoru Koketsu, Takumi Mio, Hideharu IshiharaAbstract:Reaction of selenazadienes with chloroacetyl chloride gave 1,3-Selenazole-5-carboxylic acids or 1,3-Selenazole-5-carboxylates.
Mamoru Koketsu - One of the best experts on this subject based on the ideXlab platform.
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inhibitory effects of 5 chloroacetyl 2 piperidino 1 3 Selenazole a novel selenium containing compound on skin melanin biosynthesis
Journal of Pharmacy and Pharmacology, 2010Co-Authors: Eun Joo Lee, Mamoru Koketsu, Yuji Lim, Tong Ho Kang, Chulhun Kang, Sun Yeou Kim, Jiho ParkAbstract:Objectives Increased production and accumulation of melanin leads to many hyperpigmentation disorders such as melasma, freckles and geriatric pigment spots. Thus, there is a need for the development of depigmenting agents. Based on our previous reports, selenium derivatives as anti-melanogenic lead compounds could be very important. The aim of this study was to investigate the depigmenting effect of novel selenium-containing compounds. Methods The inhibitory effects of 5-chloroacetyl-2-piperidino-1,3-Selenazole (CS1), a novel selenium-containing compound, on melanogenesis were investigated in B16F10 melanoma cells and cultured brownish guinea pig skin tissue with alpha-melanocyte-stimulating hormone stimulation. Key findings We found that CS1 inhibited melanin production in B16F10 cells by suppressing tyrosinase activity and its protein expression. In addition, Western blotting analysis revealed that CS1 suppressed the expression of tyrosinase-related protein (TRP)-1 and TRP-2. Therefore, the depigmenting effect of CS1 might have been due to inhibition of tyrosinase activity and expression of melanogenic enzymes. Furthermore, CS1 had inhibitory effects on melanin biosynthesis of primary cultured skin of brownish guinea pig. Conclusions The results suggested that CS1 could be a useful candidate for the treatment of skin hyperpigmentation.
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a facile synthesis of 2 amino 1 3 Selenazole by reaction of n n unsubstituted selenourea with ketone
Heteroatom Chemistry, 2006Co-Authors: Mamoru Koketsu, Hiromune Ando, Koichi Kanoh, Hideharu IshiharaAbstract:2-Dialkylamino-1,3-Selenazoles were yielded by the reaction of N,N-unsubstituted selenoureas with ketones in the presence of ferric chloride. © 2006 Wiley Periodicals, Inc. Heteroatom Chem 17:88–92, 2006; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20180
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a facile preparation of 2 amino 1 3 Selenazoles by reactions of n n unsubstituted selenoureas with chloroacetonitrile
Chemistry Letters, 2005Co-Authors: Mamoru Koketsu, Hidenori Tanaka, Hideharu IshiharaAbstract:Reactions of N,N-unsubstituted selenoureas 1 with chloroacetonitrile 2 was investigated. When anhydrous solvent was used, the reaction gave cyanomethyl 1-piperidinoselenocarboimidate hydrochloride 3. The reaction in solvent including water yielded 2-amino-4,5-dihydro-l,3-selenazol-4-iminium chlorides 4 in moderate to high yields.
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Facile preparation of 1,3-Selenazole-5-carboxylic acids and the carboxylates by Reaction of selenazadienes with chloroacetyl chloride
Synthesis, 2004Co-Authors: Mamoru Koketsu, Takumi Mio, Hideharu IshiharaAbstract:Reaction of selenazadienes with chloroacetyl chloride gave 1,3-Selenazole-5-carboxylic acids or 1,3-Selenazole-5-carboxylates.
Y Kumar - One of the best experts on this subject based on the ideXlab platform.
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synthesis of 2 4 disubstituted thiazoles and Selenazoles as potential antifilarial and antitumor agents 2 2 arylamido and 2 alkylamido derivatives of 2 amino 4 isothiocyanatomethyl thiazole and 2 amino 4 isothiocyanatomethyl Selenazole
Journal of Medicinal Chemistry, 1993Co-Authors: Y Kumar, Rachel Green, Dean S Wise, Linda L Wotring, Leroy B TownsendAbstract:The synthesis of a series of 2-arylamido and 2-alkylamido derivatives of 2-amino-4-(isothiocyanatomethyl)thiazole and 2-amino-4-(isothiocyanatomethyl)Selenazole is described. In vitro antiproliferative evaluations were carried out using L1210 cells. The 2-(alkylamido)thiazole derivatives were moderately antiproliferative, with IC50's of 4-8 microM. A significant increase in activity was obtained for the arylamido derivatives, with IC50's of 0.2-1 microM. The results obtained for the Selenazoles were similar to those for the thiazoles. 2-Benzamido-4-(isothiocyanatomethyl)-thiazole (19) was found to be a potent inhibitor of GMP synthetase. None of the compounds prepared in this study demonstrated antifilarial activity.
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synthesis of 2 4 disubstituted thiazoles and Selenazoles as potential antitumor and antifilarial agents 1 methyl 4 isothiocyanatomethyl thiazole 2 carbamates Selenazole 2 carbamates and related derivatives
Journal of Medicinal Chemistry, 1993Co-Authors: Y Kumar, Rachel Green, Dean S Wise, Linda L Wotring, Katherine Z Borysko, Leroy B TownsendAbstract:Methyl 4-(isothiocyanatomethyl)thiazole-2-carbamate and methyl 4-(isothiocyanatomethyl)Selenazole-2-carbamate have been prepared via chemical transformations involving 2-amino-4-(chloromethyl)thiazole (1) and 2-amino-4-(chloromethyl)Selenazole (2), respectively, as starting materials. The homoanalog, methyl 4-(2-isothiocyanatoethyl)thiazole-2-carbamate, was prepared from (2-aminothiazol-4-yl)acetic acid. All compounds prepared were evaluated for their ability to inhibit leukemia L1210 cell proliferation. Methyl 4-(isothiocyanatomethyl)thiazole-2-carbamate (7) was the most active compound in this screen, inhibiting the growth of L1210 leukemic cells with an IC50 = 3.2 microM. Mitotic blocking appears to be its primary mechanism of cytotoxic activity. Compound 7 also was the only compound which demonstrated significant in vivo antifilarial activity against the adult worms of Acanthocheilonema viteae in experimentally infected jirds. This compound was inactive against Brugia pahangi at a dosage of 100 mg/kg x 5 days.