The chemistry and biology of febrifugine and halofuginone.

abstract：:The bacterial strain Rhodococcus butanica (ATCC 21197), which exhibits nitrilase and nitrile hydratase/amidase activities, catalyses the enantioselective hydrolysis of racemic naproxen nitrile (R/S)-1 to furnish a moderate enantiomeric excess of (S)-naproxen (S)-3. Racemic naproxen amide (R/S)-2 is not a good substrat...

journal_title：Bioorganic & medicinal chemistry

authors： Effenberger F,Böhme J

更新日期：1994-07-01 00:00:00

abstract：:A series of fifteen N4-benzyl substituted 5-nitroisatin-3-thiosemicarbazones 5a-o was synthesized and evaluated for urease inhibitory, phytotoxic and cytotoxic influences. All the compounds proved to be highly potent inhibitors of the enzyme, showing inhibitory activity (IC50=0.87±0.25-8.09±0.23μM) much better than th...

journal_title：Bioorganic & medicinal chemistry

authors： Pervez H,Khan N,Zaib S,Yaqub M,Naseer MM,Tahir MN,Iqbal J

更新日期：2017-02-01 00:00:00

abstract：:Platinum-based drugs have been used for several decades to treat various cancers successfully. Cisplatin is the original compound in this class; it cross-links DNA, resulting in cell cycle arrest and cell death via apoptosis. Cisplatin is effective against several tumor types but exhibits toxic side effects; in additi...

journal_title：Bioorganic & medicinal chemistry

authors： Berger G,Leclercqz H,Derenne A,Gelbcke M,Goormaghtigh E,Nève J,Mathieu V,Dufrasne F

更新日期：2014-07-01 00:00:00

abstract：:Recent reports show that the natural beta-diketone curcumin displays important biological properties regarding the intercellular adhesion molecule-1 (ICAM-1), which plays a critical role in the immune responses and inflammation. In this study the ICAM-1 inhibitory activity of beta-diketone compounds, which are curcumi...

journal_title：Bioorganic & medicinal chemistry

authors： Caruso F,Pettinari C,Marchetti F,Rossi M,Opazo C,Kumar S,Balwani S,Ghosh B

更新日期：2009-09-01 00:00:00

abstract：:We reported previously that octadecyloxyethyl 9-(S)-[3-hydroxy-2-(phosphonomethoxy)-propyl]adenine (ODE-(S)-HPMPA) was active against genotype 1b and 2a hepatitis C virus (HCV) replicons. This is surprising because acyclic nucleoside phosphonates have been regarded as having antiviral activity only against double stra...

journal_title：Bioorganic & medicinal chemistry

authors： Valiaeva N,Wyles DL,Schooley RT,Hwu JB,Beadle JR,Prichard MN,Hostetler KY

更新日期：2011-08-01 00:00:00

abstract：:6-Hydroxymethyl-7,8-dihydropterin pyrophosphokinase (HPPK), a key enzyme in the folate biosynthetic pathway, catalyzes the pyrophosphoryl transfer from ATP to 6-hydroxymethyl-7,8-dihydropterin. The enzyme is essential for microorganisms, is absent from humans, and is not the target for any existing antibiotics. Theref...

journal_title：Bioorganic & medicinal chemistry

authors： Shi G,Shaw G,Liang YH,Subburaman P,Li Y,Wu Y,Yan H,Ji X

更新日期：2012-01-01 00:00:00

abstract：:Both histone deacetylase (HDAC) and fibroblast growth factor receptor (FGFR) are important targets for cancer therapy. Although combining dual HDAC pharmacophore with tyrosine kinase inhibitors (TKIs) had achieved a successful progress, dual HDAC/FGFR1 inhibitors haven't been reported yet. Herein, we designed a series...

journal_title：Bioorganic & medicinal chemistry

authors： Liu J,Qian C,Zhu Y,Cai J,He Y,Li J,Wang T,Zhu H,Li Z,Li W,Hu L

更新日期：2018-02-01 00:00:00

abstract：:Electronic parameters (molecular electrostatic potential MEP, charge distribution on the nitrogen atoms, dipole moment mu and ionization potential IP) were calculated by semiempirical quantum chemistry methods for 2 sets (X = H and m-CF3, the syn- and anti-rotamers of the latter being considered separately) of the 6-a...

journal_title：Bioorganic & medicinal chemistry

authors： Karolak-Wojciechowska J,Lange J,Kwiatkowski W,Gniewosz M,Plenkiewicz J

更新日期：1994-08-01 00:00:00

abstract：:A quantitative structure-activity relationship (QSAR) study has been made on two different series of tetrahydropyrimidinones acting as HIV-1 protease inhibitors. A structural parameter, the first order valence molecular connectivity index ((1)chi(v)), has been used to account for the variation in the activity. The pro...

journal_title：Bioorganic & medicinal chemistry

authors： Gayathri P,Pande V,Sivakumar R,Gupta SP

更新日期：2001-11-01 00:00:00

abstract：:A natural product inspired synthesis of 6,6,5-tricyclic compounds via a silver(I)-catalyzed formal 1,3-dipolar cycloaddition of coumarins with α-iminoesters was developed. The reaction proceeds in a stepwise reaction course under formation of the trans-substituted diastereomer with respect to the 1,3-dipole and shows ...

journal_title：Bioorganic & medicinal chemistry

authors： Potowski M,Golz C,Strohmann C,Antonchick AP,Waldmann H

更新日期：2015-06-15 00:00:00

abstract：:Four kinds of tetravalent double-headed glycoclusters [(LacNAc)4-DHGs] were designed with linkers of varying lengths consisting of alkanedioic carboxyamido groups (C6, C12, C18 and C24) between two bi-antennary LacNAc-glycosides. These glycoclusters served as high-affinity cross-linking ligands for the LacNAc-binding ...

journal_title：Bioorganic & medicinal chemistry

authors： Ogata M,Chuma Y,Yasumoto Y,Onoda T,Umemura M,Usui T,Park EY

更新日期：2016-01-01 00:00:00

abstract：:Parviflorene F (1), a novel sesquiterpenoid dimer isolated from Curcuma parviflora Wall, is a cytotoxic compound. In this study, we examined the mechanism of its cytotoxic effect in HeLa cells. Treatment with 1 enhanced the mRNA and protein expression of TRAIL-R2 (tumor necrosis factor alpha-related apoptosis inducing...

journal_title：Bioorganic & medicinal chemistry

authors： Ohtsuki T,Tamaki M,Toume K,Ishibashi M

更新日期：2008-02-15 00:00:00

abstract：:A novel series of thaizole and oxazole containing phenoxy acetic acid derivatives is reported as PPAR-pan agonists. Incorporation of structurally constrained oxime-ether based linker in the chemotype of a potent PPARδ selective agonist GW-501516 was adapted as designing strategy. In vitro, selected test compounds 12a,...

journal_title：Bioorganic & medicinal chemistry

authors： Makadia P,Shah SR,Pingali H,Zaware P,Patel D,Pola S,Thube B,Priyadarshini P,Suthar D,Shah M,Giri S,Trivedi C,Jain M,Patel P,Bahekar R

更新日期：2011-01-15 00:00:00

abstract：:In the present study, we report that three new lupane triterpenes (1-3), in addition to 16 known ones (4-19), were isolated from the root bark of Maytenus cuzcoina and the leaves of Maytenus chiapensis. Their structures were elucidated by spectral analysis, including homonuclear and heteronuclear correlation NMR exper...

journal_title：Bioorganic & medicinal chemistry

authors： Reyes CP,Núñez MJ,Jiménez IA,Busserolles J,Alcaraz MJ,Bazzocchi IL

更新日期：2006-03-01 00:00:00

abstract：:Replacing the naphthalene C-unit of the anti-tuberculosis drug bedaquiline with a range of bicyclic heterocycles of widely differing lipophilicity gave analogs with a 4.5-fold range in clogP values. The biological results for these compounds indicate on average a lower clogP limit of about 5.0 in this series for reten...

journal_title：Bioorganic & medicinal chemistry

authors： Sutherland HS,Tong AST,Choi PJ,Conole D,Blaser A,Franzblau SG,Cooper CB,Upton AM,Lotlikar MU,Denny WA,Palmer BD

更新日期：2018-05-01 00:00:00

abstract：:Adenosine A1 receptors are attracting great interest as drug targets for their role in cognitive deficits. Antagonism of the adenosine A1 receptor may offer therapeutic benefits in complex neurological diseases, such as Alzheimer's and Parkinson's disease. The aim of this study was to discover potential selective aden...

journal_title：Bioorganic & medicinal chemistry

authors： Van der Walt MM,Terre'Blanche G

更新日期：2015-10-15 00:00:00

abstract：:Within our efforts in the discovery of novel potent and selective ligands for the FXR receptor, 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine was synthesized and evaluated for its ability to activate and modulate the biological response of the receptor. Alphascreen and RT-PCR revealed that...

journal_title：Bioorganic & medicinal chemistry

authors： Gioiello A,Macchiarulo A,Carotti A,Filipponi P,Costantino G,Rizzo G,Adorini L,Pellicciari R

更新日期：2011-04-15 00:00:00

abstract：:Synthesis and pharmacological characterisation of a series of compounds in which the oxime substructure present in imoproxifan was constrained in the pentatomic NO-donor furoxan ring, as well as their structurally related furazan analogues devoid of NO-donating properties, are described. The whole series of products d...

journal_title：Bioorganic & medicinal chemistry

authors： Tosco P,Bertinaria M,Di Stilo A,Cena C,Sorba G,Fruttero R,Gasco A

更新日期：2005-08-01 00:00:00

abstract：:A growing number of proteins are known to exert their regulatory or biological functions via RNA binding. In some cases genetic interactions allow us to infer candidate targets for RNA directed regulation, but in many other cases identification of potential regulatory targets is problematic. We have developed an in vi...

journal_title：Bioorganic & medicinal chemistry

authors： Brunel C,Ehresmann B,Ehresmann C,McKeown M

更新日期：2001-10-01 00:00:00

abstract：:One of the grand challenges in chemical biology is identifying a small-molecule modulator for each individual function of all human proteins. Instead of targeting one protein at a time, an efficient approach to address this challenge is to target entire protein families by taking advantage of the relatively high level...

journal_title：Bioorganic & medicinal chemistry

authors： Areias FM,Brea J,Gregori-Puigjané E,Zaki ME,Carvalho MA,Domínguez E,Gutiérrez-de-Terán H,Proença MF,Loza MI,Mestres J

更新日期：2010-05-01 00:00:00

abstract：:Vascular Adhesion Protein-1 (VAP-1) is a promising therapeutic target for the treatment of several inflammatory-related diseases including diabetic microvascular complication. We identified glycine amide derivative 3 as a novel structure with moderate VAP-1 inhibitory activity. Structure-activity relationship studies ...

journal_title：Bioorganic & medicinal chemistry

authors： Yamaki S,Suzuki D,Fujiyasu J,Neya M,Nagashima A,Kondo M,Akabane T,Kadono K,Moritomo A,Yoshihara K

更新日期：2017-01-01 00:00:00

abstract：:2-Amino-6-fluoro-9-(4-hydroxy-3-hydroxymethylbut-1-yl)purine (7), and its mono- and diesters 8-15 were prepared and evaluated for their potential as prodrugs of penciclovir. Treatment of 2-amino-6-chloro-9-(4-hydroxy-3-hydroxymethylbut-1-yl)purine (5) with trimethylamine in THF followed by a reaction of the resulting ...

journal_title：Bioorganic & medicinal chemistry

authors： Kim DK,Lee N,Kim HT,Im GJ,Kim KH

更新日期：1999-03-01 00:00:00

abstract：:Bromodomain-containing protein 4 (BRD4) is a key epigenetic regulator in cancer, and inhibitors targeting BRD4 exhibit great anticancer activity. By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4 inhibitors were designed and synthesi...

journal_title：Bioorganic & medicinal chemistry

authors： Li Q,Li J,Cai Y,Zou Y,Chen B,Zou F,Mo J,Han T,Guo W,Huang W,Qiu Q,Qian H

更新日期：2020-08-01 00:00:00

abstract：:In recent years, special attention has been paid to the A3 adenosine receptor (A3AR) as a possible pharmacological target to treat intestinal inflammation. In this work, it was set up a novel method to quantify the concentration of a promising anti-inflammatory agent inside and outside of intestinal barrier using the ...

journal_title：Bioorganic & medicinal chemistry

authors： Buccioni M,Dal Ben D,Lambertucci C,Martí Navia A,Ricciutelli M,Spinaci A,Volpini R,Marucci G

更新日期：2019-08-01 00:00:00

abstract：:12-O-β-D-glucopyranosyl jasmonic acid (JAG) shows unique biological activities, including leaf-closing of Samanea saman. It is expected that the mode of action for such regulation is distinct from that of other jasmonates. We developed high-performance compact molecular probes (CMPs) based on JAG that can be used for ...

journal_title：Bioorganic & medicinal chemistry

authors： Ueda M,Yang G,Ishimaru Y,Itabashi T,Tamura S,Kiyota H,Kuwahara S,Inomata S,Shoji M,Sugai T

更新日期：2012-10-01 00:00:00

abstract：:We have synthesized 3-hydroxy- and 3,4,5-trihydroxypipecolic acid derivatives corresponding to 5-aza derivatives of uronic acids and evaluated their inhibitory activities against various glycosidases including beta-glucuronidase. Compounds 4 and 5 were chosen as common intermediates for the synthesis of 3,4,5-trihydro...

journal_title：Bioorganic & medicinal chemistry

authors： Yoshimura Y,Ohara C,Imahori T,Saito Y,Kato A,Miyauchi S,Adachi I,Takahata H

更新日期：2008-09-01 00:00:00

abstract：:To date, J-113397 represents the most potent and selective non peptide NOP receptor antagonist widely used in pharmacological studies. However, the synthesis, purification, and enantiomer separation of this molecule, which contains two chiral centers, is rather difficult and low-yielding. Here, we synthesized and test...

journal_title：Bioorganic & medicinal chemistry

authors： Trapella C,Guerrini R,Piccagli L,Calo' G,Carra' G,Spagnolo B,Rubini S,Fanton G,Hebbes C,McDonald J,Lambert DG,Regoli D,Salvadori S

更新日期：2006-02-01 00:00:00

abstract：:A new meso-2,4,6-trimethoxyphenyl porphyrin covalently linked to a 2',6'-dinitro-4'-trifluoromethylphenyl group by an amine bond 5 and its metal complex with Cd(II) 6 was prepared. The photodynamic activities of 5 and 6 were evaluated in vitro on Hep-2 cells. A considerable increase in the photocytotoxic effect was fo...

journal_title：Bioorganic & medicinal chemistry

authors： Milanesio ME,Morán FS,Yslas EI,Alvarez MG,Rivarola V,Durantini EN

更新日期：2001-08-01 00:00:00

abstract：:Two types of structural variants of D-myo-inositol 1,4,5-trisphosphate [Ins(1,4,5)P3] were prepared by a chemoenzymatic route. These 6-O-substituted analogues retained the biological activity of Ins(1,4,5)P3, and were able to elicit Ca2+ release from porcine brain microsomes. Moreover, these derivatives allowed the pr...

journal_title：Bioorganic & medicinal chemistry

authors： Gou DM,Shieh WR,Lu PJ,Chen CS

更新日期：1994-01-01 00:00:00

abstract：:Pin1 (Protein interacting with NIMA1) is a peptidyl prolyl cis-trans isomerase (PPIase) which specifically catalyze the conformational conversion of the amide bond of pSer/Thr-Pro motifs in its substrate proteins and is a novel promising anticancer target. A series of new thiazole derivatives were designed and synthes...

journal_title：Bioorganic & medicinal chemistry

authors： Zhao H,Cui G,Jin J,Chen X,Xu B

更新日期：2016-11-15 00:00:00