Identification and evaluation of a napyradiomycin as a potent Nrf2 activator: Anti-oxidative and anti-inflammatory activities.

abstract：:Deregulation of many kinases is directly linked to cancer development and the tyrosine kinase family is one of the most important targets in current cancer therapy regimens. In this study, we have designed and synthesized a series of thieno[2,3-d]pyrimidine derivatives as an EGFR and HER2 tyrosine kinase inhibitors. A...

journal_title：Bioorganic chemistry

authors： Elmetwally SA,Saied KF,Eissa IH,Elkaeed EB

更新日期：2019-07-01 00:00:00

abstract：:Models have been developed for the interaction of the pyrrolo[1,2-a]benzimidazole (PBI) antitumor agents with the two-electron activating enzyme DT-diaphorase and the DNA major groove. The DT-diaphorase model and experimental results indicate that the S-enantiomer of 3-carbamido PBI can enantioselect ovarian cancers. ...

journal_title：Bioorganic chemistry

authors： Huang X,Suleman A,Skibo EB

更新日期：2000-12-01 00:00:00

abstract：:Succinimides are well recognized heterocyclic compounds in drug discovery which produce diverse therapeutically related applications in pharmacological practices. Researches in medicinal chemistry field have isolated and synthesized succinimide derivatives with multiple medicinal properties including anticonvulsant, a...

journal_title：Bioorganic chemistry

authors： Zhao Z,Yue J,Ji X,Nian M,Kang K,Qiao H,Zheng X

更新日期：2020-12-15 00:00:00

abstract：:Several new 5,6-dihydropyrimidine-2(1H)-thione derivatives have been prepared and investigated for their potencies for anticonvulsant activity against maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) test in mice. The acute neurotoxicity was measured by rotarod test. Compounds 3c and 3l were foun...

journal_title：Bioorganic chemistry

authors： Sahu M,Siddiqui N,Iqbal R,Sharma V,Wakode S

更新日期：2017-10-01 00:00:00

abstract：:Analkali tolerant α-l-rhamnosidase has been purified to homogeneity from the culture filtrate of a new fungal strain, Fusarium moniliforme MTCC-2088, using concentration by ultrafiltration and cation exchange chromatography on CM cellulose column. The molecular mass of the purified enzyme has been found to be 36.0 kDa...

journal_title：Bioorganic chemistry

authors： Kumar D,Yadav S,Yadava S,Yadav KDS

更新日期：2019-03-01 00:00:00

abstract：:Based on a report that sulfanylphthalimides are highly potent monoamine oxidase (MAO) B selective inhibitors, the present study examines the adenosine receptor affinities and MAO-B inhibitory properties of a series of 4- and 5-sulfanylphthalimide analogues. Since adenosine antagonists (A1 and A2A subtypes) and MAO-B i...

journal_title：Bioorganic chemistry

authors： Van der Walt MM,Terre'Blanche G,Petzer A,Petzer JP

更新日期：2015-04-01 00:00:00

abstract：:The stilbenoid resveratrol (1) was subjected to regioselective acetylation catalysed by Candida antarctica lipase (CAL) to obtain 4'-acetylresveratrol (2). CAL biocatalysed regioselective alcoholysis of 3,5,4'-triacetylresveratrol (3), 3,5,4'-tributanoylresveratrol (6), and 3, 4, 5'-trioctanoylresveratrol (9) afforded...

journal_title：Bioorganic chemistry

authors： Cardile V,Lombardo L,Spatafora C,Tringali C

更新日期：2005-02-01 00:00:00

abstract：:The reactions of a ribonuclease model substrate, the compound uridine-3'-p-nitrophenyl phosphate, have been examined using heavy-atom isotope effects and stereochemical analysis. The cyclization of this compound is subject to catalysis by general base (by imidazole buffer), specific base (by carbonate buffer), and by ...

journal_title：Bioorganic chemistry

authors： Hengge AC,Bruzik KS,Tobin AE,Cleland WW,Tsai MD

更新日期：2000-06-01 00:00:00

abstract：:Starting from the compound (3,4-dimethoxyphenyl)(2-(3,4-dimethoxyphenyl)cyclopent-1-en-1-yl)methanone (4), two diols and three tetrol derivatives were synthesised. Morover, from the reactions of 1,3-dimethoxybenzene and 1,4-dimethoxybenzene with adipoyl chloride, fifteen new along with nine known compounds were obtain...

journal_title：Bioorganic chemistry

authors： Artunc T,Menzek A,Taslimi P,Gulcin I,Kazaz C,Sahin E

更新日期：2020-07-01 00:00:00

abstract：:Seven new diterpenoids (1-7), including five 7-membered ring vibsane-type diterpenoids, vibsanolide A-E (1-5) and a pair of epimers of 14,15,16,17-tetranorvibsane-type diterpenoids possessing bicyclo[4.2.1]nonane moiety, vibsanolide F-G (6-7), together with twelve known analogues (8-19) were isolated from the crude ex...

journal_title：Bioorganic chemistry

authors： Li SF,Yu XQ,Li YL,Bai M,Lin B,Yao GD,Song SJ

更新日期：2021-01-01 00:00:00

abstract：:The non-mevalonate or 2-C-methyl-d-erythritol-4-phosphate (MEP) pathway is responsible for generating isoprenoid precursors in plants, protozoa, and bacteria. Because this pathway is absent in humans, its enzymes represent potential targets for the development of herbicides and antibiotics. 1-Deoxy-d-xylulose (DXP) re...

journal_title：Bioorganic chemistry

authors： Murkin AS,Manning KA,Kholodar SA

更新日期：2014-12-01 00:00:00

abstract：:A series of monomeric tetrahedral complexes of stoichiometry, [MX(HL)(Ph3P)2] (In case of M = Cu, H1L, X = I, 1; Br, 2; Cl, 3; H3L, X = I, 4; Br, 5; Cl, 6; H4L, X = I, 7; Br, 8; Cl, 9 and in case of M = Ag, H1L, X = Cl, 13; Br, 14; H2L, X = Cl, 15, Br 16; H3L, X = Cl, 17, Br, 18) were synthesized by the reaction of co...

journal_title：Bioorganic chemistry

authors： Khan A,Jasinski JP,Smolenski VA,Hotchkiss EP,Kelley PT,Shalit ZA,Kaur M,Paul K,Sharma R

更新日期：2018-10-01 00:00:00

abstract：:A series of novel naproxen analogues containing 3-aryl-1,2,4-oxadiazoles moiety (4b-g) and their reaction intermediates aryl carboximidamides moiety (3b-g) was synthesized and evaluated in vitro as dual COXs/15-LOX inhibitors. Compounds 3b-g exhibited superior inhibitory activity than celecoxib as COX-2 inhibitors. Co...

journal_title：Bioorganic chemistry

authors： Youssif BGM,Mohamed MFA,Al-Sanea MM,Moustafa AH,Abdelhamid AA,Gomaa HAM

更新日期：2019-04-01 00:00:00

abstract：:Dibrefeldins A and B (1 and 2), two unexpected brefeldin A (BFA) dimers, as well as brefeldin F (3), brefeldin G (4), and 14-hydroxy-BFA (5), three new BFA derivatives, together with three new naturally occurring BFA derivatives (6-8) and four known analogues (9-12), were isolated from the fungus Penicillium janthinel...

journal_title：Bioorganic chemistry

authors： Zeng F,Chen C,Al Chnani AA,Zhou Q,Tong Q,Wang W,Zang Y,Gong J,Wu Z,Liu J,Wang J,Zhu H,Zhang Y

更新日期：2019-05-01 00:00:00

abstract：:The marine environment remains a rich source for the discovery and development of novel bioactive compounds. The present paper describes the design, synthesis and biological evaluation of a library of small molecule heterocyclic mimetics of the marine 2,5-diketopiperazine barettin which is a powerful natural antioxida...

journal_title：Bioorganic chemistry

authors： Labrière C,Andersen JH,Albrigtsen M,Hansen JH,Svenson J

更新日期：2019-03-01 00:00:00

abstract：:Focal adhesion kinase (FAK) is an intracellular non-receptor tyrosine kinase responsible for development of various tumor types. Aiming to explore new potent inhibitors, two series of 2,4-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives were designed and synthesized on the base of structure-based design strategy....

journal_title：Bioorganic chemistry

authors： Wang R,Zhao X,Yu S,Chen Y,Cui H,Wu T,Hao C,Zhao D,Cheng M

更新日期：2020-09-01 00:00:00

abstract：:A series of novel 2-substituted quinoline-4-carboxylic acids was synthesized by Doebner reaction starting from freely available protocatechuic aldehyde and vanillin precursors. Human dihydroorotate dehydrogenase (hDHODH) was recognised as a clear molecular target for these heterocycles. All compounds were also tested ...

journal_title：Bioorganic chemistry

authors： Petrović MM,Roschger C,Chaudary S,Zierer A,Mladenović M,Jakovljević K,Marković V,Botta B,Joksović MD

更新日期：2020-12-01 00:00:00

abstract：:P-glycoprotein (P-gp) is one of the cell membrane pumps which mediate the efflux of molecules such as anticancer drugs to the extracellular matrix of tumor cells. P_gp is a member of the ATP-binding cassette (ABC) transporter family that is implicated in cancer multidrug resistance (MDR). Since MDR is a contributor to...

journal_title：Bioorganic chemistry

authors： Mollazadeh S,Sahebkar A,Kalalinia F,Behravan J,Hadizadeh F

更新日期：2019-10-01 00:00:00

abstract：:Three series of arylbenzimidazole derivatives 3-40, 45 have been simply synthesized and tested for their antioxidant capacity. The 2-arylbenzimidazoles were tested against various radicals by the DPPH, FRAP and ORAC tests and showed different activity profiles. It has been observed that the number and position of the ...

journal_title：Bioorganic chemistry

authors： Baldisserotto A,Demurtas M,Lampronti I,Tacchini M,Moi D,Balboni G,Pacifico S,Vertuani S,Manfredini S,Onnis V

更新日期：2020-01-01 00:00:00

abstract：:Crataegus pinnatifida has been famous for its nutritional purpose. However, systematic investigation on the bioactive constituents is still lacking, although this fruit has been reported for its cytotoxic effect before. In this study, two pairs of new lignan enantiomers (1a/1b, 2a/2b), which isolated using chiral chro...

journal_title：Bioorganic chemistry

authors： Shang XY,Guo R,Yu XQ,Lin B,Huang XX,Yao GD,Song SJ

更新日期：2020-11-01 00:00:00

abstract：:Five previously undescribed 4,5-seco-abietane rearrange diterpenoids (1-5, Prionidipene A-E) were isolated from the aerial parts of Salvia prionitis, along with thirteen known seco-abietane diterpenoids (6-18). The structures of 1-5 were elucidated mainly based on analysis of NMR and MS data. The absolute configuratio...

journal_title：Bioorganic chemistry

authors： Li L,Zhou M,Xue G,Wang W,Zhou X,Wang X,Kong L,Luo J

更新日期：2018-12-01 00:00:00

abstract：:Inspired with an increasing environmental awareness, we performed an eco-friendly amenable process for the synthesis of silver nanoparticles (AgNPs) using the catkins of Piper longum as an alternative approach with the existing methods of using plant extracts. The fabrication of nanoparticles occurred within 10 min. T...

journal_title：Bioorganic chemistry

authors： Huang H,Shan K,Liu J,Tao X,Periyasamy S,Durairaj S,Jiang Z,Jacob JA

更新日期：2020-10-01 00:00:00

abstract：:A novel group of 1,3,4-oxadaiazoles, a group known for their anti-inflammatory activity, is hybridized with nitric oxide (NO) releasing group, oxime, for its gastro-protective action and potential synergistic effect. The synthesized hybrids were evaluated for their anti-inflammatory, analgesic, antioxidant and ulcerog...

journal_title：Bioorganic chemistry

authors： Abd-Ellah HS,Abdel-Aziz M,Shoman ME,Beshr EA,Kaoud TS,Ahmed AF

更新日期：2016-12-01 00:00:00

abstract：:The ability to custom-make fluorescent sensors for different analytes could have a tremendous impact in a variety of areas. Template-directed polymerization or molecular imprinting seems to be a promising approach for the preparation of high-affinity and specific binding sites for different template molecules. However...

journal_title：Bioorganic chemistry

authors： Gao S,Wang W,Wang B

更新日期：2001-10-01 00:00:00

abstract：:Aldose reductase (AR) catalyzes the NADPH-dependent reduction of glucose to sorbitol in the polyol pathway, which plays an important role in the development of diabetic complications including cataract, retinopathy, nephropathy, and neuropathy. AR has been considered as an important target to heal these long-term diab...

journal_title：Bioorganic chemistry

authors： Sever B,Altıntop MD,Demir Y,Akalın Çiftçi G,Beydemir Ş,Özdemir A

更新日期：2020-09-01 00:00:00

abstract：:Four series of para or meta - substituted thiazolylbenzenesulfonamides bearing Cl substituents were designed, synthesized, and evaluated as inhibitors of all 12 catalytically active recombinant human carbonic anhydrase (CA) isoforms. Observed affinities were determined by the fluorescent thermal shift assay and the in...

journal_title：Bioorganic chemistry

authors： Čapkauskaitė E,Zubrienė A,Paketurytė V,Timm DD,Tumkevičius S,Matulis D

更新日期：2018-04-01 00:00:00

abstract：:Phosphatidylinositol 3-kinase (PI3K) pathway regulates various cellular processes, such as proliferation, growth, autophagy and apoptosis. Class I PI3K is frequently mutated and overexpressed in a lot of human cancers and PI3K was considered as a target for therapeutic treatment of cancer. In this study, we designed a...

journal_title：Bioorganic chemistry

authors： Ding HW,Yu L,Bai MX,Qin XC,Song MT,Zhao QC

更新日期：2019-12-01 00:00:00

abstract：:In this work we describe not previously explored binding studies on the reversible interaction of benzoxaborole with ligands of medical and pharmaceutical interest such as nucleosidic drugs gemcitabine and capecitabine, as well as the hydrophobic chemotherapeutic doxorubicin. We include functional derivatives of benzo...

journal_title：Bioorganic chemistry

authors： Samaniego Lopez C,Martínez JH,Acebedo SL,Spagnuolo CC

更新日期：2019-09-01 00:00:00

abstract：:Steroids are polycyclic compounds that have a wide range of biological activities. They are bio-synthesized from cholesterol through a series of enzyme-mediated transformations, so they are highly lipophilic and readily enter most cells to interact with intracellular receptors, making them ideal vehicles for targeting...

journal_title：Bioorganic chemistry

authors： Tantawy MA,Nafie MS,Elmegeed GA,Ali IAI

更新日期：2017-08-01 00:00:00

abstract：:The paper highlighted quinoxalines as potent ligands to corticotropin-releasing factor receptor types 1 and 2. The content includes design and structure-activity relationship of 50 model substances to CRFR1, CRFR2α and CRF2β, respectively. It is important to bear in mind, that our concept has based on challenging rese...

journal_title：Bioorganic chemistry

authors： Ivanova B,Spiteller M

更新日期：2015-02-01 00:00:00