Development of polymeric drug delivery system for recognizing vascular endothelial dysfunction.

abstract：:Small molecules are central players in chemical biology studies. They promote the perturbation of cellular processes underlying diseases and enable the identification of biological targets that can be validated for therapeutic intervention. Small molecules have been shown to accurately tune a single function of plurip...

journal_title：Bioorganic & medicinal chemistry

authors： Abet V,Mariani A,Truscott FR,Britton S,Rodriguez R

更新日期：2014-08-15 00:00:00

abstract：:Ten 1-phenyl-1H-pyrazolo[3,4-b]pyridine derivatives connected by a linker group to benzenesulfonamide moieties with different substituents in the 4-position were synthesized and assayed against Plasmodium falciparum. These ten compounds exhibited activity in vitro against the chloroquine-resistant clone W2 with IC50 v...

journal_title：Bioorganic & medicinal chemistry

authors： Silva TB,Bernardino AMR,Ferreira MLG,Rogerio KR,Carvalho LJM,Boechat N,Pinheiro LCS

更新日期：2016-09-15 00:00:00

abstract：:Chemical investigation of the organic extract obtained from the sponge Plakortis simplex collected in the South China Sea afforded five new polyketide endoperoxides (2 and 4-7), along with two known analogues (1 and 3). The stereostructures of these metabolites have been deduced on the basis of spectroscopic analysis ...

journal_title：Bioorganic & medicinal chemistry

authors： Chianese G,Persico M,Yang F,Lin HW,Guo YW,Basilico N,Parapini S,Taramelli D,Taglialatela-Scafati O,Fattorusso C

更新日期：2014-09-01 00:00:00

abstract：:A series of 6-amino-4-oxo-1,3-diphenyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl derivatives was synthesized. The compounds demonstrated to be novel, potent and selective inhibitors of Interleukin-8-induced human neutrophil chemotaxis. A SAR study was performed by varying the carbonyl function at position 5 and...

journal_title：Bioorganic & medicinal chemistry

authors： Cesarini S,Spallarossa A,Ranise A,Bruno O,Arduino N,Bertolotto M,Dallegri F,Tognolini M,Gobbetti T,Barocelli E

更新日期：2009-05-15 00:00:00

abstract：:The present study describes the chemical synthesis and pharmacological evaluation of a new series of eleven compounds stereoisomers of imidobenzenesulfonylaziridines in the forced-swimming test (FST) in mice. The pharmacological results of these compounds show that six of them, given intraperitoneally, reduced the imm...

journal_title：Bioorganic & medicinal chemistry

authors： Duarte FS,Andrade Eda S,Vieira RA,Uieara M,Nunes RJ,de Lima TC

更新日期：2006-08-01 00:00:00

abstract：:The crystal structure of ABT-378 (lopinavir), bound to the active site of HIV-1 protease is described. A comparison with crystal structures of ritonavir, A-78791, and BILA-2450 shows some analogous features with previous reported compounds. A cyclic urea unit in the P(2) position of ABT-378 is novel and makes two bide...

journal_title：Bioorganic & medicinal chemistry

authors： Stoll V,Qin W,Stewart KD,Jakob C,Park C,Walter K,Simmer RL,Helfrich R,Bussiere D,Kao J,Kempf D,Sham HL,Norbeck DW

更新日期：2002-08-01 00:00:00

abstract：:Bioassay-guided fractionation of a cytotoxic EtOAc extract of the fungal strain, Chaetomium globosum, inhabiting the rhizosphere of the Christmas cactus, Opuntia leptocaulis, of the Sonoran desert afforded a new dihydroxanthenone, globosuxanthone A (1), a new tetrahydroxanthenone, globosuxanthone B (2), two new xantho...

journal_title：Bioorganic & medicinal chemistry

authors： Wijeratne EM,Turbyville TJ,Fritz A,Whitesell L,Gunatilaka AA

更新日期：2006-12-01 00:00:00

abstract：:In our ongoing program aimed at deeply investigating the endocannabinoid system (ES), a set of new alkyl-resorcinol derivatives was prepared focusing on the nature and the importance of the carboxamide functionality. Binding studies on CB1 and CB2 receptors, monoacylglycerol lipase (MAGL) and fatty acid amide hydrolas...

journal_title：Bioorganic & medicinal chemistry

authors： Brizzi A,Aiello F,Marini P,Cascio MG,Corelli F,Brizzi V,De Petrocellis L,Ligresti A,Luongo L,Lamponi S,Maione S,Pertwee RG,Di Marzo V

更新日期：2014-09-01 00:00:00

abstract：:Four kaempferol glycosides were isolated from the leaves of Cinnamomum osmophloeum Kaneh, a Taiwan endemic tree. These compounds namely, kaempferitrin (1), kaempferol 3-O-beta-D-glucopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-7-O-alpha-L-rhamnopyranoside (2), kaempferol 3-O-beta-D-apiofuranosyl-(1-->2)-alpha-L-arabinof...

journal_title：Bioorganic & medicinal chemistry

authors： Fang SH,Rao YK,Tzeng YM

更新日期：2005-04-01 00:00:00

abstract：:1,11-Didechloro-6-methyl-4'-O-demethyl rebeccamycin (JDC-108), a rebeccamycin analog possessing potent anti-tumor activities, was prepared via a concise one-pot strategy in good yield. The interaction between JDC-108 and human serum albumin (HSA) was studied by spectroscopic methods including fluorescence spectroscopy...

journal_title：Bioorganic & medicinal chemistry

authors： Cui F,Qin L,Zhang G,Liu X,Yao X,Lei B

更新日期：2008-08-15 00:00:00

abstract：:A fluorescent cyclodextrin-Tb(III) complex is successfully synthesized and can include bile salts in its hydrophobic cavities. Therefore, it can efficiently induce the secondary assembly of small bile salt primary micelles to large micelle aggregates, and the aggregation process can be easily observed by transmission ...

journal_title：Bioorganic & medicinal chemistry

authors： Liu Y,Zhang N,Chen Y,Chen GS

更新日期：2006-10-01 00:00:00

abstract：:The effects of Brazilian green propolis ethanol extract on Cry j1-induced cys-leukotrienes and histamine release from peripheral leukocytes of patients with allergic rhinitis were investigated. One of the key mechanisms for the anti-allergic properties of the extract was revealed to be the suppression of cys-LTs relea...

journal_title：Bioorganic & medicinal chemistry

authors： Tani H,Hasumi K,Tatefuji T,Hashimoto K,Koshino H,Takahashi S

更新日期：2010-01-01 00:00:00

abstract：:Inhibitors of transglycosylases may serve as potent antibiotics that are less prone to resistance development in bacterial pathogens. To facilitate the search of such compounds, a transglycosylase (TGase) domain of the membrane integral multidomain Streptococcus pneumoniae PBP1b was cloned and expressed. This TGase do...

journal_title：Bioorganic & medicinal chemistry

authors： Liu H,Wong CH

更新日期：2006-11-01 00:00:00

abstract：:The trans-2,3-disubstituted piperidine, quinazolinone-containing natural product febrifugine (also known as dichroine B) and its synthetic analogue, halofuginone, possess antimalarial activity. More recently studies have also shown that halofuginone acts as an agent capable of reducing fibrosis, an indication with cli...

journal_title：Bioorganic & medicinal chemistry

authors： McLaughlin NP,Evans P,Pines M

更新日期：2014-04-01 00:00:00

abstract：:A series of potential DNA-binding antitumor agents, 2-[omega-(alkylamino)alkyl]-9-methoxy-5-nitro-2,6-dihydroindazolo[4,3-bc][1,5]naphthyridines (2a-f), 10-aza derivatives of PZA, has been prepared by condensation of 9-chloro-2-methoxy-6-nitro-5,10-dihydrobenzo[b][1,5]naphthyridin-10-one (6) with the appropriate (omeg...

journal_title：Bioorganic & medicinal chemistry

authors： Magnano A,Sparapani S,Lucciarini R,Michela M,Amantini C,Santoni G,Antonini I

更新日期：2004-11-15 00:00:00

abstract：:A series of xanomeline analogs were synthesized and evaluated for binding at the M(1) muscarinic acetylcholine receptor (M(1) receptor). Specifically, compounds that substitute the O-hexyl chain of xanomeline with polar, ionizable, or conformationally restricted moieties were assessed for their ability to bind to the ...

journal_title：Bioorganic & medicinal chemistry

authors： Kane BE,Grant MK,El-Fakahany EE,Ferguson DM

更新日期：2008-02-01 00:00:00

abstract：:Opioid compounds with mixed micro agonist/delta antagonist properties could be used as analgesics with low propensity to induce tolerance and dependence. Here we report the synthesis of a new designed multiple ligand deriving from the micro selective agonist endomorphin-2 and the delta selective antagonist pharmacopho...

journal_title：Bioorganic & medicinal chemistry

authors： Salvadori S,Trapella C,Fiorini S,Negri L,Lattanzi R,Bryant SD,Jinsmaa Y,Lazarus LH,Balboni G

更新日期：2007-11-15 00:00:00

abstract：:A novel series of acetamide-substituted derivatives and two prodrugs of doravirine were designed and synthesized as potent HIV-1 NNRTIs by employing the structure-based drug design strategy. In MT-4 cell-based assays using the MTT method, it was found that most of the new compounds exhibited moderate to excellent inhi...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Z,Yu Z,Kang D,Zhang J,Tian Y,Daelemans D,De Clercq E,Pannecouque C,Zhan P,Liu X

更新日期：2019-02-01 00:00:00

abstract：:The in vitro antitumor activities of 2,6-di-[2-(heteroaryl)vinyl]pyridines versus the standard National Cancer Institute 60 cell lines panel and of 2,6-di-[2-(heteroaryl)vinyl] pyridinium cations versus MCF7 (human mammary carcinoma) and LNCap (prostate carcinoma) cell lines are reported. Antiproliferative effects in ...

journal_title：Bioorganic & medicinal chemistry

authors： Barresi V,Condorelli DF,Fortuna CG,Musumarra G,Scirè S

更新日期：2002-09-01 00:00:00

abstract：:Conflicts with the notion that specific substrate interactions were required in the control of reaction path in active transport systems, P-glycoprotein showed extraordinarily low specificity. Therefore, overexpression P-glycoprotein excluded a large number of anticancer agents from cancer cells, and multidrug resista...

journal_title：Bioorganic & medicinal chemistry

authors： Xu W,Chen S,Wang X,Wu H,Yamada H,Hirano T

更新日期：2020-06-15 00:00:00

abstract：:Positron emission tomography (PET) using fluorine-18 (18F)-labeled 2-nitroimidazole radiotracers has proven useful for assessment of tumor oxygenation. However, the passive diffusion-driven cellular uptake of currently available radiotracers results in slow kinetics and low tumor-to-background ratios. With the aim to ...

journal_title：Bioorganic & medicinal chemistry

authors： Wanek T,Kreis K,Križková P,Schweifer A,Denk C,Stanek J,Mairinger S,Filip T,Sauberer M,Edelhofer P,Traxl A,Muchitsch VE,Mereiter K,Hammerschmidt F,Cass CE,Damaraju VL,Langer O,Kuntner C

更新日期：2016-11-01 00:00:00

abstract：:Concise total syntheses of (R)- and (S)-argentilactone have been developed via enantioselective catalytic allylation (ECA) and ring-closing metathesis pathways (four steps, 39% overall yield and 82-84% ee) from 2-octynal and their in vitro activity against cancer cells is described. ...

journal_title：Bioorganic & medicinal chemistry

authors： de Fatima A,Kohn LK,Antônio MA,de Carvalho JE,Pilli RA

更新日期：2004-10-15 00:00:00

abstract：:The induction of differentiation represents a new and promising approach to cancer therapy, well illustrated by the treatment of acute promyelocytic leukemia (APL) with 1,25-dihydroxyvitamin D3 [1,25-(OH)2D3] or all-trans retinoic acid (ATRA). Using combinations of low, nontoxic concentrations of either 1,25-(OH)2D3 o...

journal_title：Bioorganic & medicinal chemistry

authors： Kim SH,Kim SW,Choi SJ,Kim YC,Kim TS

更新日期：2006-10-01 00:00:00

abstract：:Tertiary sulfonamidomethyl esters of benzylpenicillin (4) were synthesised and evaluated as a new class of potential prodrugs for beta-lactam antibiotics. Their hydrolysis in aqueous buffers was studied by HPLC and reveal a U-shaped pH rate profile with a pH-independent process extending from ca. pH 2 to ca. pH 10. Th...

journal_title：Bioorganic & medicinal chemistry

authors： Iley J,Barroso H,Moreira R,Lopes F,Calheiros T

更新日期：2000-07-01 00:00:00

abstract：:Twelve thiorhodamine derivatives have been examined for their ability to stimulate the ATPase activity of purified human P-glycoprotein (P-gp)-His(10), to promote uptake of calcein AM and vinblastine into multidrug-resistant, P-gp-overexpressing MDCKII-MDR1 cells, and for their rates of transport in monolayers of mult...

journal_title：Bioorganic & medicinal chemistry

authors： Orchard A,Schamerhorn GA,Calitree BD,Sawada GA,Loo TW,Claire Bartlett M,Clarke DM,Detty MR

更新日期：2012-07-15 00:00:00

abstract：:The AP sites are representative of DNA damage and known as an intermediate in the base excision repair (BER) pathway which is involved in the repair of damaged nucleobases by reactive oxygen species, UVA irradiation, and DNA alkylating agents. Therefore, it is expected that the inhibition or modulation of the AP site ...

journal_title：Bioorganic & medicinal chemistry

authors： Abe YS,Sasaki S

更新日期：2019-12-15 00:00:00

abstract：:A novel series of fluorinated 2-phenylindole derivatives were synthesized and evaluated as β-amyloid imaging probes for PET. The in vitro inhibition assay demonstrated that their binding affinities for Aβ(1-42) aggregates ranged from 28.4 to 1097.8 nM. One ligand was labeled with (18)F ([(18)F]1a) for its high affinit...

journal_title：Bioorganic & medicinal chemistry

authors： Fu H,Yu L,Cui M,Zhang J,Zhang X,Li Z,Wang X,Jia J,Yang Y,Yu P,Jia H,Liu B

更新日期：2013-07-01 00:00:00

abstract：:T22 ([Tyr5,12,Lys7]-polyphemusin II) has been shown to have strong anti-human immunodeficiency virus (HIV) activity comparable to that of 3'-azido-2',3'-dideoxythymidine (AZT). T22, an 18-residue peptide amide, takes an antiparallel beta-sheet structure that is maintained by two disulfide bridges. Herein we synthesize...

journal_title：Bioorganic & medicinal chemistry

authors： Tamamura H,Waki M,Imai M,Otaka A,Ibuka T,Waki K,Miyamoto K,Matsumoto A,Murakami T,Nakashima H,Yamamoto N,Fujii N

更新日期：1998-04-01 00:00:00

abstract：:A series of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides bearing the halogens iodine and bromine were synthesised and their binding affinity for the peripheral benzodiazepine binding sites (PBBS) in rat kidney mitochondrial membranes was evaluated using [(3)H]PK11195. Central benzodiazepine receptor (CBR) affinities we...

journal_title：Bioorganic & medicinal chemistry

authors： Homes TP,Mattner F,Keller PA,Katsifis A

更新日期：2006-06-01 00:00:00

abstract：:A new series of pyrano chalcone derivatives containing indole moiety (3-42, 49a-49r) were synthesized and evaluated for their antiproliferative activities. Among all the compounds, compound 49b with a propionyloxy group at the 4-position of the left phenyl ring and N-methyl-5-indoly on the right ring displayed the mos...

journal_title：Bioorganic & medicinal chemistry

authors： Wang G,Li C,He L,Lei K,Wang F,Pu Y,Yang Z,Cao D,Ma L,Chen J,Sang Y,Liang X,Xiang M,Peng A,Wei Y,Chen L

更新日期：2014-04-01 00:00:00