abstract：:Macrocyclic bis(bibenzyl)-type phenolic natural products, found exclusively in bryophytes, exhibit potent antibacterial activity towards methicillin-resistant Staphylococcus aureus (anti-MRSA activity). Here, in order to identify the minimum essential structure for cell membrane leakage-mediated anti-MRSA activity of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujii K,Morita D,Onoda K,Kuroda T,Miyachi H

更新日期：2016-05-01 00:00:00

abstract：:We report structure-guided modifications of the benzyloxy substituent of the Insulin-like Growth Factor-1 Receptor (IGF-1R) inhibitor NVP-AEW541. This chemical group has been shown to confer selectivity against other protein kinases but at the expense of a metabolism liability. X-ray crystallography has revealed that ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Stauffer F,Cowan-Jacob SW,Scheufler C,Furet P

更新日期：2016-04-15 00:00:00

abstract：:The bacterial repair enzyme MutT hydrolyzes the damaged nucleotide OdGTP (the 5'-triphosphate derivative of 8-oxo-2'-deoxyguanosine; OdG), which is a known mutagen and has been linked to antibacterial action. Previous work has indicated important roles for the C8-oxygen, N7-hydrogen, and C2-exocyclic amine during OdGT...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hamm ML,McFadden EJ,Ghio M,Lindell MA,Gerien KS,O'Handley SF

更新日期：2016-04-15 00:00:00

abstract：:Atractylodes macrocephula Koidz (A. macrocephula, also known as Baizhu) is an important ingredient in several traditional Chinese herb complexes for the treatment of abdominal pain and gastroenterology diseases for thousands of years. We previously demonstrated the induction of ROS-mediated apoptosis by methanol extra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang HL,Lin TW,Huang YL,Huang RL

更新日期：2016-04-15 00:00:00

abstract：:A series of anilinonicotinyl linked pyrazolo[1,5-a]pyrimidine conjugates (6a-x) were synthesized and evaluated for their antiproliferative activity. Some of these conjugates exhibited promising cytotoxic effects in the MCF-7 cell line and among these 6a and 6c exhibited significant effects, apart from G2/M cell cycle ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kamal A,Faazil S,Hussaini SM,Ramaiah MJ,Balakrishna M,Patel N,Pushpavalli SN,Pal-Bhadra M

更新日期：2016-04-15 00:00:00

abstract：:The novel analysis method consisting of size-exclusion chromatography (SEC) and HRMS analysis was firstly applied in the discovery of potential inhibitors towards cancer drug targets. With vascular endothelial growth factor receptor (VEGFR-2) as a target, dynamic combinatorial libraries (DCLs) were prepared by reactin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang Z,Fang Z,He W,Wang Z,Gan H,Tian Q,Guo K

更新日期：2016-04-01 00:00:00

abstract：:Gynostemma pentaphyllum has been widely used as a traditional herb for its antioxidant and immunostimulatory activities. We have previously reported several useful dammarane-type saponins with cytotoxicity against A549 human lung cancer cells from heat-processed G. pentaphyllum. In this study, a new dammarane-type sap...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xing SF,Jang M,Wang YR,Piao XL

更新日期：2016-04-01 00:00:00

abstract：:A series of 1,3,4-oxadiazol-2-ones was synthesized and tested for activity as antagonists at GPR55 in cellular beta-arrestin redistribution assays. The synthesis was designed to be modular in nature so that a sufficient number of analogues could be rapidly accessed to explore initial structure-activity relationships. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Meza-Aviña ME,Lingerfelt MA,Console-Bram LM,Gamage TF,Sharir H,Gettys KE,Hurst DP,Kotsikorou E,Shore DM,Caron MG,Rao N,Barak LS,Abood ME,Reggio PH,Croatt MP

更新日期：2016-04-01 00:00:00

abstract：:In this study, a series of bis(4-hydroxy)benzophenone oxime ether derivatives such as 12c, 12e and 12h were identified as novel estrogen receptor (ER) agonists that have additional and complementary anti-proliferative activities via ER-independent mechanism in cancer cells. These compounds are expected to overcome the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim T,Kim HI,An JY,Lee J,Lee NR,Heo J,Kim JE,Yu J,Lee YS,Inn KS,Kim NJ

更新日期：2016-04-01 00:00:00

abstract：:The transcription factor nuclear factor-κB (NF-κB) controls many physiological processes including inflammation, immunity, and apoptosis. In this study, a novel series of 6-phenoxy-[1,2,4]triazolo[3,4-a]phthalazine-3-carboxamide derivatives were synthesized as potent anti-inflammatory agents, which acted on tumor necr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu DC,Gong GH,Wei CX,Jin XJ,Quan ZS

更新日期：2016-03-15 00:00:00

abstract：:In a search of small molecules active against apoptosis-resistant cancer cells, a series of isatin-based heterocyclic compounds were synthesized and found to inhibit proliferation of cancer cell lines resistant to apoptosis. The synthesis of these compounds involved a condensation of commercially available, active met...

journal_title：Bioorganic & medicinal chemistry letters

authors： Evdokimov NM,Magedov IV,McBrayer D,Kornienko A

更新日期：2016-03-15 00:00:00

abstract：:The objective of this study was to develop a positron emission tomography (PET) probe with hypoxia targeting specificity and a relatively long half-life. The synthesis, (64)Cu-labeling in vitro and in vivo study of the novel 2-nitroimidazole complex (64)Cu-BMS2P2 is presented in this study. The hypoxia targeting capac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Luo Z,Zhu H,Lin X,Chu T,Luo R,Wang Y,Yang Z

更新日期：2016-03-01 00:00:00

abstract：:From an easily available partially protected formal derivative of 1-deoxymannojirimycin, by hydroxymethyl chain-branching and further elaboration, lipophilic analogs of the powerful β-d-galactosidase inhibitor 4-epi-isofagomine have become available. New compounds exhibit improved inhibitory activities comparable to b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thonhofer M,Weber P,Santana AG,Fischer R,Pabst BM,Paschke E,Schalli M,Stütz AE,Tschernutter M,Windischhofer W,Withers SG

更新日期：2016-03-01 00:00:00

abstract：:Eight new isocoumarin glycosides (1-8) were obtained from the solid culture of the wetland soil-derived fungus Metarhizium anisopliae (No. DTH12-10). Their chemical structures were elucidated by analyses of HR ESI-TOF MS, (1)H, (13)C NMR, (1)H-(1)H COSY, HSQC, and HMBC spectra. The absolute configurations were determi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tian JF,Li PJ,Li XX,Sun PH,Gao H,Liu XZ,Huang P,Tang JS,Yao XS

更新日期：2016-03-01 00:00:00

abstract：:Investigations of a biaryl ether scaffold identified tetrahydronaphthalene Raf inhibitors with good in vivo activity; however these compounds had affinity toward the hERG potassium channel. Herein we describe our work to eliminate this hERG activity via alteration of the substituents on the benzoic amide functionality...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang SC,Adhikari S,Afroze R,Brewer K,Calderwood EF,Chouitar J,England DB,Fisher C,Galvin KM,Gaulin J,Greenspan PD,Harrison SJ,Kim MS,Langston SP,Ma LT,Menon S,Mizutani H,Rezaei M,Smith MD,Zhang DM,Gould AE

更新日期：2016-02-15 00:00:00

abstract：:Prostate cancer is the most frequently diagnosed cancer and is one of the leading causes of male cancer death in the world. Recently, in the course of our screening for a novel anticancer compound, we synthesized carbocyclic analogs of pyrrolo[2,3-d]pyrimidine nucleoside; compounds 5, and 6. In the current study, we r...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suh H,Choi KW,Lee J,Ryou C,Rhee H,Lee CH

更新日期：2016-02-15 00:00:00

abstract：:The essential oils from leaves of Piper malacophyllum (Piperaceae) showed to be mainly composed by two alkenylphenol derivatives: gibbilimbols A and B. After isolation and structural characterization by NMR and MS data analysis, both compounds were evaluated against promastigote/amastigote forms of Leishmania (L.) inf...

journal_title：Bioorganic & medicinal chemistry letters

authors： Varela MT,Dias RZ,Martins LF,Ferreira DD,Tempone AG,Ueno AK,Lago JH,Fernandes JP

更新日期：2016-02-15 00:00:00

abstract：:The structure of the S1P2 antagonist 1 has been modified with the aim of improving its oral bioavailability. The chemical modification of the alkyl chain and carboxylic acid moieties of 1 led to significant improvements in the oral exposure of compounds belonging to this series. The optimization of the ring size of th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kusumi K,Shinozaki K,Yamaura Y,Hashimoto A,Kurata H,Naganawa A,Otsuki K,Matsushita T,Sekiguchi T,Kakuuchi A,Yamamoto H,Seko T

更新日期：2016-02-15 00:00:00

abstract：:The recent success of vemurafenib shows the importance of selective BRAF V600E inhibition in melanoma. However, paradoxical activation by structurally diverse ATP-competitive RAF kinase inhibitors strongly suggests that selective CRAF inhibitors, not BRAF inhibitors, would be ideal for some Ras mutation cancer treatme...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aman W,Lee J,Kim M,Yang S,Jung H,Hah JM

更新日期：2016-02-15 00:00:00

abstract：:DNA polymerases can efficiently and sequence selectively incorporate oligonucleotide (ODN)-modified nucleotides and the incorporated oligonucleotide strand can be employed as primer in rolling circle amplification (RCA). The effective amplification of the DNA primer by Φ29 DNA polymerase allows the sequence-selective ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Verga D,Welter M,Marx A

更新日期：2016-02-01 00:00:00

abstract：:The histone methylation on lysine residues is one of the most studied post-translational modifications, and its aberrant states have been associated with many human diseases. In 2012, Kruidenier et al. reported GSK-J1 as a selective Jumonji H3K27 demethylase (JMJD3 and UTX) inhibitor. However, there is limited informa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hu J,Wang X,Chen L,Huang M,Tang W,Zuo J,Liu YC,Shi Z,Liu R,Shen J,Xiong B

更新日期：2016-02-01 00:00:00

abstract：:Protein-protein interactions (PPIs) are key elements of several important biological processes and have emerged as valuable targets in medicinal chemistry. Importantly, numerous specific protein-protein interactions (e.g., p53-HDM2 and Bcl-2-BH3 domains) were found to be involved in the development of several diseases...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wójcik P,Berlicki Ł

更新日期：2016-02-01 00:00:00

abstract：:The 1',6'-isomer of neplanocin A possesses biological properties that have not been optimised through rationally conceived analogues. In that direction, this Letter reports the use of the Ullmann reaction to achieve enantiomeric 3-deaza-1',6'-isoneplanocin and 3-bromo-3-deaza-1',6'-isoneplanocin. These four compounds ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu C,Chen Q,Schneller SW

更新日期：2016-02-01 00:00:00

abstract：:The seminal human dopamine D3 receptor (hD3R) ligand BP 897 has shown interesting properties during clinical trials. However, its lack of selectivity towards human adrenergic receptor impedes further development. Two approaches were followed to increase hD3R selectivity. The lead optimisation succeeded, we disclose he...

journal_title：Bioorganic & medicinal chemistry letters

authors： Capet M,Calmels T,Levoin N,Danvy D,Berrebi-Bertrand I,Stark H,Schwartz JC,Lecomte JM

更新日期：2016-02-01 00:00:00

abstract：:Exploring copper(I)- and ruthenium(II)-catalyzed azide-alkyne cycloadditions and a Sonogashira protocol, novel cytostatic ferrocene-cinchona hybrids were synthetized displaying significant in vitro activity on HepG-2 and HT-29 cells. Preliminary SAR studies disclosed that compounds incorporating linkers with 1,2,3-tri...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kocsis L,Szabó I,Bősze S,Jernei T,Hudecz F,Csámpai A

更新日期：2016-02-01 00:00:00

abstract：:Considering the therapeutic potential of fatty acid amides, the present study aimed to evaluate their in vitro activity against Toxocara canis larvae and their cytotoxicity for the first time. Linoleylpyrrolidilamide was the most potent, with a minimal larvicidal concentration (MLC) of 0.05 mg/mL and 27% cytotoxicity ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mata-Santos T,D'Oca CDRM,Mata-Santos HA,Fenalti J,Pinto N,Coelho T,Berne ME,da Silva PEA,D'Oca MGM,Scaini CJ

更新日期：2016-02-01 00:00:00

abstract：:Bcl homologs prominently contribute to apoptotic resistance in cancer cells and serve as molecular targets in treatment of various cancers. Herein, we report the synthesis of biphenyl-adamantane derivatives by a ligand free palladium on carbon based Suzuki reaction using diisopropylamine as a base for the coupling of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Anusha S,Mohan CD,Ananda H,Baburajeev CP,Rangappa S,Mathai J,Fuchs JE,Li F,Shanmugam MK,Bender A,Sethi G,Basappa,Rangappa KS

更新日期：2016-02-01 00:00:00

abstract：:In an effort to rapidly access vancomycin analogues bearing diverse functionality at the 6c-Cl (the 'in-chloride') position, a two-step dechlorination/cross-coupling protocol was developed. Conditions for efficient cross-coupling of the relatively unreactive 6c-Cl group were found that ensure high conversion with mini...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wadzinski TJ,Gea KD,Miller SJ

更新日期：2016-02-01 00:00:00

abstract：:Two series of 5-phenyl furocoumarin derivatives were designed and prepared based on our previous research. All new compounds were characterized by (1)H NMR, (13)C NMR and mass spectra. Furthermore, they were screened for their vasodilatory activity on the mesenteric artery of Sprague-Dawley rats, and they all presente...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang C,Wang T,Huang L,Lu W,Zhang J,He H

更新日期：2016-01-15 00:00:00

abstract：:A series of novel quinoline-oxadiazole hybrid compounds was designed based on stepwise rational modification of the lead molecules reported previously, in order to enhance bioactivity and improve druglikeness. The hybrid compounds synthesized were screened for biological activity against Mycobacterium tuberculosis H37...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jain PP,Degani MS,Raju A,Anantram A,Seervi M,Sathaye S,Ray M,Rajan MGR

更新日期：2016-01-15 00:00:00

abstract：:Two novel compounds with mannose-derived structure, bearing a tetrazole (compound 3) and a sulfone group (compound 4) in terminal position, have been prepared from methyl α-d-mannopyranoside in reduced number of steps. The angiogenic activity of 3 and 4 has been screened using the chick chorioallantoic membrane (CAM) ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ionescu C,Sippelli S,Toupet L,Barragan-Montero V

更新日期：2016-01-15 00:00:00

abstract：:New derivatives of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124, 3), were synthesized as continuation to our previous patented efforts. Compounds 15 and 20 showed marginal hypnotic potency compared to 3. Compounds 15 (0.78mmol/kg) and 20 (0.39mmol/kg) showed remarkable 100% protec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Al-Rashood STA,Hassan GS,El-Messery SM,El-Taher KEH,Hefnawy MM,Al-Omar MA,El-Subbagh HI

更新日期：2016-01-15 00:00:00

abstract：:ADX88178 (1) has been recently developed as a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4). The aim of this study was to develop [(11)C]1 as a novel positron emission tomography ligand and to evaluate its binding ability for mGluR4. Using stannyl precursor 3, [(11)C]1 was efficie...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujinaga M,Yamasaki T,Nengaki N,Ogawa M,Kumata K,Shimoda Y,Yui J,Xie L,Zhang Y,Kawamura K,Zhang MR

更新日期：2016-01-15 00:00:00

abstract：:Oxomollugin (2) is a degradation product of mollugin (1) and a potent inhibitor of NO-production including nuclear factor kappa B signals. In our endeavor to develop a potent anti-inflammatory compound, we synthesized several aza-derivatives of oxomollugin (2) and evaluated their NO-production inhibitory activity. Aza...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nishino H,Nakajima Y,Kakubari Y,Asami N,Deguchi J,Nugroho AE,Hirasawa Y,Kaneda T,Kawasaki Y,Goda Y,Morita H

更新日期：2016-01-15 00:00:00

abstract：:Biflorin 1 is a biologically active quinone, isolated from Capraria biflora. Five new biflorin-based nitrogen derivatives were synthesized, of which two were mixtures of (E)- and (Z)- isomers: (Z)-2a, (Z)-2b, (Z)-3a, (Z)- and (E)-3b, (Z)- and (E)-3c. The antibacterial activity was investigated using the microdilution ...

journal_title：Bioorganic & medicinal chemistry letters

authors： da S Souza LG,Almeida MCS,Lemos TLG,Ribeiro PRV,de Brito ES,Silva VLM,Silva AMS,Braz-Filho R,Costa JGM,Rodrigues FFG,Barreto FS,de Moraes MO

更新日期：2016-01-15 00:00:00

abstract：:Pretomanid (PA-824) is an important nitroimidazole antitubercular agent in late stage clinical trials. However, pretomanid is limited by poor solubility and high protein binding, which presents opportunities for improvement in its physiochemical properties. Conversely, the oxazolidinone linezolid has excellent physico...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rakesh,Bruhn DF,Scherman MS,Singh AP,Yang L,Liu J,Lenaerts AJ,Lee RE

更新日期：2016-01-15 00:00:00

abstract：:Two novel acridone-quinoline alkaloids, acriquinoline A (1) and acriquinoline B (2), together with twenty-two known compounds were isolated from the methanol extract of the root of Citrus reticulata Blanco. The structures of all compounds were determined by comprehensive analyses of their 1D and 2D NMR and mass spectr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fomani M,Ngeufa Happi E,Nouga Bisoue A,Ndom JC,Kamdem Waffo AF,Sewald N,Wansi JD

更新日期：2016-01-15 00:00:00

abstract：:Recently, we had identified an unexplored pocket adjacent to the known binding site of allosteric MEK inhibitors which allowed us to design highly potent and in vivo efficacious novel inhibitors. We now report that our initial preclinical candidate, featuring a phenoxy side chain with a sulfamide capping group, displa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hartung IV,Hammer S,Hitchcock M,Neuhaus R,Scholz A,Siemeister G,Bohlmann R,Hillig RC,Pühler F

更新日期：2016-01-01 00:00:00

abstract：:A series of novel 3-substituted isocoumarins was prepared via Pd-catalysed coupling processes and screened in vitro for antifungal activity against Candida species. The study revealed antifungal potential of isocoumarins possessing the azole substituents, which, in some cases, showed biological properties equal to tho...

journal_title：Bioorganic & medicinal chemistry letters

authors： Simic M,Paunovic N,Boric I,Randjelovic J,Vojnovic S,Nikodinovic-Runic J,Pekmezovic M,Savic V

更新日期：2016-01-01 00:00:00

abstract：:N-Aryl derivatives of edaravone were identified as potentially effective small molecule inhibitors of tau and beta-amyloid aggregation in the context of developing disease-modifying therapeutics for Alzheimer's disease (AD). Palladium-catalyzed hydrazine monoarylation protocols were then employed as an expedient means...

journal_title：Bioorganic & medicinal chemistry letters

authors： MacLean MA,Diez-Cecilia E,Lavery CB,Reed MA,Wang Y,Weaver DF,Stradiotto M

更新日期：2016-01-01 00:00:00