Sensitive and selective viral DNA detection assay via microbead-based rolling circle amplification.

abstract：:Kynurenine monooxygenase (KMO) is a potential drug target for treatment of neurodegenerative disorders such as Huntington's and Alzheimer's diseases. We have evaluated substituted kynurenines as substrates or inhibitors of KMO from Cytophaga hutchinsonii. Kynurenines substituted with a halogen at the 5-position are ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Phillips RS,Anderson AD,Gentry HG,Güner OF,Bowen JP

更新日期：2017-04-15 00:00:00

abstract：:Metabolites of the potent DP antagonist, MK-0524, were generated using in vitro systems including hepatic microsomes and hepatocytes. Four metabolites (two hydroxylated diastereomers, a ketone and an acyl glucuronide) were characterized by LC-MS/MS and 1H NMR. Larger quantities of these metabolites were prepared by ei...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nicoll-Griffith DA,Seto C,Aubin Y,Lévesque JF,Chauret N,Day S,Silva JM,Trimble LA,Truchon JF,Berthelette C,Lachance N,Wang Z,Sturino C,Braun M,Zamboni R,Young RN

更新日期：2007-01-15 00:00:00

abstract：:Coexpression of EGFR and HER2 has been found in many tumors such as breast, ovarian, colon and prostate cancers, with poor prognosis of the patients. Herein, our team has designed and synthesized new eighteen compounds with 6-substituted 4-anilinoquinazoline core to selectively inhibit EGFR/HER2 tyrosine kinases. Twel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Elkamhawy A,Farag AK,Viswanath AN,Bedair TM,Leem DG,Lee KT,Pae AN,Roh EJ

更新日期：2015-11-15 00:00:00

abstract：:New polyphenol classes have been tested against amyloid-beta peptide aggregation. We have identified four novel polyphenols which could be efficient fibril inhibitors in Alzheimer's disease: malvidin and its glucoside and curculigosides B and D. We suggest that molecules with the particular C(6)-linkers-C(6) structure...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rivière C,Richard T,Vitrac X,Mérillon JM,Valls J,Monti JP

更新日期：2008-01-15 00:00:00

abstract：:N-(Dansylamino)hexylaminocarbonylpentyl-1,5-dideoxy-1,5-imino-D-galactitol, a strong competitive inhibitor of β-galactosidase, enhances residual β-galactosidase activities in fibroblasts and serves as lead en route to diagnostic compounds for tracking the fate of mutant β-gal as well as aberrant GM1 gangliosides by li...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fröhlich RF,Fantur K,Furneaux RH,Paschke E,Stütz AE,Wicki J,Withers SG,Wrodnigg TM

更新日期：2011-11-15 00:00:00

abstract：:Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective and orally active mPGES-1 inhibitors. These inhibitors are significantly more potent than the previously reported chlorophenanthrene imidazole 1 (MF63) with a human whole blood IC50 of 0.20 and 0.14 microM, respectively. It exhibited a s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Giroux A,Boulet L,Brideau C,Chau A,Claveau D,Côté B,Ethier D,Frenette R,Gagnon M,Guay J,Guiral S,Mancini J,Martins E,Massé F,Méthot N,Riendeau D,Rubin J,Xu D,Yu H,Ducharme Y,Friesen RW

更新日期：2009-10-15 00:00:00

abstract：:The reduced activation of PPARs has a positive impact on cancer cell growth and viability in multiple preclinical tumor models, suggesting a new therapeutic potential for PPAR antagonists. In the present study, the benzothiazole amides 2a-g were synthesized and their activities on PPARs were investigated. Transactivat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ammazzalorso A,De Lellis L,Florio R,Laghezza A,De Filippis B,Fantacuzzi M,Giampietro L,Maccallini C,Tortorella P,Veschi S,Loiodice F,Cama A,Amoroso R

更新日期：2019-08-15 00:00:00

abstract：:The in vitro antimycobacterial activity of cobalt(II) and copper(II) complexes of some fluorinated isonicotinoylhydrazones was evaluated in a TB-infected macrophage model; all metalcomplexes exhibited excellent activity against Mycobacterium tuberculosis Erdman growing within macrophages, at concentrations much lower ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Maccari R,Ottanà R,Bottari B,Rotondo E,Vigorita MG

更新日期：2004-12-06 00:00:00

abstract：:A regiochemical and stereochemical mixture of flexible linkers bearing terminal azide functionality was synthesized in two steps from squalene and was used to connect two high affinity NDP-alpha-MSH ligands or two low affinity MSH(4) ligands. The ligands were N-terminally acylated using N-hydroxysuccinimidoyl 5-hexyno...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jagadish B,Sankaranarayanan R,Xu L,Richards R,Vagner J,Hruby VJ,Gillies RJ,Mash EA

更新日期：2007-06-15 00:00:00

abstract：:Virtual screening, a fast, computational approach to identify drug leads [Perola, E.; Xu, K.; Kollmeyer, T. M.; Kaufmann, S. H.; Prendergast, F. G. J. Med. Chem.2000, 43, 401; Miller, M. A. Nat. Rev. Drug Disc.2002, 1 220], is limited by a known challenge in crystallographically determining flexible regions of protein...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dooley AJ,Shindo N,Taggart B,Park JG,Pang YP

更新日期：2006-02-15 00:00:00

abstract：:The resistance of pathogenic fungi and failure of drug therapy increased dramatically. Numerous studies have reported the individual or synergistic antifungal potency of natural and synthesized flavonoids, especially against drug-resistant fungi. This brief review summarizes the structure and individual or synergistic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin YS

更新日期：2019-10-01 00:00:00

abstract：:Beauveria bassiana AM278 and Absidia coerulea AM93 converted 8-prenylnaringenin (1) into two glycoside derivatives (7-O-β-D-glucopyranoside) (2) and 7-O-β-D-4'''-O-methylglucopyranoside) (3) in high yields in processes conducted in Saboraud medium. 8-Prenylnaringenin 7-O-β-D-4'''-O-methylglucopyranoside (3) is a new c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bartmańska A,Tronina T,Huszcza E

更新日期：2012-10-15 00:00:00

abstract：:Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites. In order to reduce attrition due to metabolism-induced toxicity and to improve the safety of drug candidates, we developed a simple cell viability assay by combining a bioactivation system (huma...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rana P,Will Y,Nadanaciva S,Jones LH

更新日期：2016-08-15 00:00:00

abstract：:Obesity is a chronic medical condition that is affecting large population throughout the world. CB1 as a target for treatment of obesity has been under intensive studies. Taranabant was discovered and then developed by Merck as the 1st generation CB1R inverse agonist. Reported here is part of our effort on the 2nd gen...

journal_title：Bioorganic & medicinal chemistry letters

authors： Du W,Jewell JP,Lin LS,Colandrea VJ,Xiao JC,Lao J,Shen CP,Bateman TJ,Reddy VB,Ha SN,Shah SK,Fong TM,Hale JJ,Hagmann WK

更新日期：2009-09-01 00:00:00

abstract：:Cynaropicrin is a guaianolide sesquiterpene lactone, which has potent in vitro and in vivo inhibitory activity against Trypanosoma brucei, the protozoan parasite that causes human African trypanosomiasis (HAT; sleeping sickness). Herein, we describe the synthesis of cynaropicrin's deuterated derivative, cynaropicrin-d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sato T,Hara S,Sato M,Ogawa K,Adams M,Usuki T

更新日期：2015-12-01 00:00:00

abstract：:We have developed a new series of progesterone receptor modulators based upon the 4-aryl-phenylsulfonamide. Initial work in the series afforded potent compounds with good properties, however an advanced intermediate proved to be genotoxic in a non-GLP Ames assay following metabolic activation. We subsequently solved t...

journal_title：Bioorganic & medicinal chemistry letters

authors： McComas C,Cohen J,Huselton C,Marella M,Melenski E,Mugford C,Slayden O,Winneker R,Wrobel J,Yudt MR,Fensome A

更新日期：2012-12-01 00:00:00

abstract：:A phytochemical study on the roots of Pongamia pinnata afforded five new isoflavone and isoflavanone derivatives (1-5), including two previously undescribed phenylisoflavones possessing an 1,2-oxetane ring, along with 21 known compounds (6-26) among which compound 18 is the first time to be isolated from nature. The s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wen R,Lv H,Jiang Y,Tu P

更新日期：2018-04-01 00:00:00

abstract：:Twenty three side chain analogs of the crambescidin alkaloids were prepared from the corresponding pentacyclic zwitterionic core acid. In the crambescidin 800 and 657 series, potency increased with increasing chain length. In addition, substantial variations in tumor selectivity with structure were seen. Crambescidin ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aron ZD,Pietraszkiewicz H,Overman LE,Valeriote F,Cuevas C

更新日期：2004-07-05 00:00:00

abstract：:The Hotoda's sequence substituted with TBDPS via 5'-end nucleobase existed as parallel quadruplex structure and exhibited inhibitory activities in an HIV-1 envelop proteins mediated cell-cell fusion assay. This result demonstrated that the 5'-aromatic groups of the Hotoda's sequence are allowed to have a large spatial...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen W,Xu L,Cai L,Zheng B,Wang K,He J,Liu K

更新日期：2011-10-01 00:00:00

abstract：:The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park CH,Choe H,Jang IY,Kwon SY,Latif M,Lee HK,Lee HJ,Yang EH,Yun JI,Chae CH,Cho SY,Choi SU,Ha JD,Jung H,Kim HR,Kim P,Lee CO,Yun CS,Lee K

更新日期：2013-11-15 00:00:00

abstract：:Here we report the model studies of the reactions between NADH models (using HEH and BNAH) and sulfane sulfurs (using polysulfides). Such reactions could lead to the oxidation of NADH models and the production of hydrogen sulfide (H2S). Kinetics of the reaction between BNAH and elemental sulfur S8 were determined in e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Peng B,Liu C,Li Z,Day JJ,Lu Y,Lefer DJ,Xian M

更新日期：2017-02-01 00:00:00

abstract：:2-Phenyl-4-piperidinyl-6,7-dihydrothieno[3,4-d]pyrimidine derivative (2) was found to be a new PDE4 inhibitor with moderate PDE4B activity (IC50=150 nM). A number of derivatives with a variety of 4-amino substituents and fused bicyclic pyrimidines were synthesized. Among these, 5,5-dioxo-7,8-dihydro-6H-thiopyrano[3,2-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Goto T,Shiina A,Yoshino T,Mizukami K,Hirahara K,Suzuki O,Sogawa Y,Takahashi T,Mikkaichi T,Nakao N,Takahashi M,Hasegawa M,Sasaki S

更新日期：2013-06-01 00:00:00

abstract：:Our internal casein kinase 1ε lead inhibitor, compound 1 was partially cleared by the polymorphic cytochrome P450 2D6. CYP2D6 involvement in metabolism implies more extensive clinical trials. We therefore wanted to reduce the contribution to clearance by this enzyme. We utilized metabolism reports for compound 1 perfo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vaz RJ,Li Y,Metz M,Yang D,Shen H,Munson M

更新日期：2018-12-15 00:00:00

abstract：:Various 1,3,4-oxadiazole derivatives have been synthesized and their antiproliferative properties have been studied. The in vitro screening was performed against androgen dependent (LNCaP) and androgen independent (PC-3) prostate cancer cell lines. Most of the compounds showed promising activity. Among them, compounds...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mochona B,Qi X,Euynni S,Sikazwi D,Mateeva N,Soliman KF

更新日期：2016-06-15 00:00:00

abstract：:Hydroxy urea moieties are introduced as a new class of bradykinin B(1) receptor antagonists. First, the SAR of the lead compound was systematically explored. Subsequent optimization resulted in the identification of several biaryl-based hydroxyurea bradykinin B(1) receptor antagonists with low-nanomolar activity and v...

journal_title：Bioorganic & medicinal chemistry letters

authors： Schnatbaum K,Schaudt M,Stragies R,Pfeifer JR,Gibson C,Locardi E,Scharn D,Richter U,Kalkhof H,Dinkel K,Zischinsky G

更新日期：2010-02-01 00:00:00

abstract：:Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best enzyme potency and cellular selectivity. Changes made to the 6-furanyl group had little impact on the enzyme a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Petrov KG,Zhang YM,Carter M,Cockerill GS,Dickerson S,Gauthier CA,Guo Y,Mook RA Jr,Rusnak DW,Walker AL,Wood ER,Lackey KE

更新日期：2006-09-01 00:00:00

abstract：:Cu(II) complexes with 4,6-di(tert-butyl)-2-aminophenol (I) and 2-anilino-4,6-di(tert-butyl)phenol (II) have been synthesized and characterized by means of elemental analysis, TG/DTA, FT-IR, UV-vis, ESR, and conductance measurements. The compounds I and II can coordinate in their singly deprotonated forms and behave as...

journal_title：Bioorganic & medicinal chemistry letters

authors： Loginova NV,Koval'chuk TV,Zheldakova RA,Osipovich NP,Sorokin VL,Polozov GI,Ksendzova GA,Glushonok GK,Chernyavskaya AA,Shadyro OI

更新日期：2006-10-15 00:00:00

abstract：:Three new polyhydroxytriterpenoid derivatives, 23-O-neochebuloylarjungenin 28-O-β-d-glycopyranosyl ester (1), 23-O-4'-epi-neochebuloylarjungenin (2), and 23-O-galloylpinfaenoic acid 28-O-β-d-glucopyranosyl ester (17) were isolated from the fruits of Terminalia chebula Retz. along with fourteen known ones. Their struct...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee DY,Yang H,Kim HW,Sung SH

更新日期：2017-01-01 00:00:00

abstract：:A series of thiazolo[4,5-d]pyrimidine thiones and -ones was prepared and discovered to have good binding affinity to the CRH-R1 receptor, thus showing promise as a new class of potential anxiolytics and/or antidepressants. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Beck JP,Curry MA,Chorvat RJ,Fitzgerald LW,Gilligan PJ,Zaczek R,Trainor GL

更新日期：1999-04-19 00:00:00

abstract：:A computational approach was utilized to study the relative binding modes of diospyrin (bisnaphthoquinonoid) with the crystal structure of human DNA-TopoI and the recently reported Leishmania donavani DNA-TopoI. Additionally, the binding site interactions of amino derivatives of diospyrin with human TopoI were studied...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chhabra S,Sharma P,Ghoshal N

更新日期：2007-08-15 00:00:00