Synthesis and biological evaluation of radioiodinated 3-phenylcoumarin derivatives targeting myelin in multiple sclerosis.

abstract：:Structural features from the anticancer prodrug nemorubicin (MMDX) and the DNA-binding molecule DRAQ5™ were used to prepare anthraquinone-based compounds, which were assessed for their potential to interrogate cytochrome P450 (CYP) functional activity and localisation. 1,4-disubstituted anthraquinone 8 was shown to be...

journal_title：Bioorganic & medicinal chemistry letters

authors： Errington RJ,Sadiq M,Cosentino L,Wiltshire M,Sadiq O,Sini M,Lizano E,Pujol MD,Morais GR,Pors K

更新日期：2018-05-01 00:00:00

abstract：:A group of tri and tetrasubstituted urea derivatives have been found to be hH(3)-antagonists. The most potent compounds were found in the class of (piperazine-1-yl)-(piperidine-1-yl)-methanones which in addition showed negligible hERG inhibition. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lau JF,Jeppesen CB,Rimvall K,Hohlweg R

更新日期：2006-10-15 00:00:00

abstract：:A new class of tumor necrosis factor alpha (TNF-alpha) synthesis inhibitors based on a N-2,4-pyrimidine-N-phenyl-N'-alkyl urea scaffold is described. Many of these compounds showed low-nanomolar activity against lipopolysaccharide stimulated TNF-alpha production. Two analogs were tested in an in vivo rat iodoacetate m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Maier JA,Brugel TA,Clark MP,Sabat M,Golebiowski A,Bookland RG,Laufersweiler MJ,Laughlin SK,Vanrens JC,De B,Hsieh LC,Brown KK,Juergens K,Walter RL,Janusz MJ

更新日期：2006-07-01 00:00:00

abstract：:In our continuous efforts to identify and develop novel targeted cancer treatments, a new morpholino-thiazole scaffold active against PI3Kβ has been identified. This Letter reports the optimization of this compound class to develop PI3Kβ isoform-selective inhibitors with suitable pharmacological properties. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Certal V,Halley F,Virone-Oddos A,Filoche-Rommé B,Carry JC,Gruss-Leleu F,Bertin L,Guizani H,Pilorge F,Richepin P,Karlsson A,Charrier V,Abecassis PY,Vincent L,Nicolas JP,Lengauer C,Garcia-Echeverria C,Schio L

更新日期：2014-03-15 00:00:00

abstract：:Effect of a series of 1-phenylthioureas 1a-k and 1,3-disubstituted thioureas 2a-k were evaluated against melanin formation in melanoma B16 cell line and mushroom tyrosinase. Inhibitory activity of tyrosinase of 1-phenylthioureas 1a-k is parallel to their melanogenic inhibition. Thus, the melanogenic inhibition in mela...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thanigaimalai P,Lee KC,Sharma VK,Joo C,Cho WJ,Roh E,Kim Y,Jung SH

更新日期：2011-11-15 00:00:00

abstract：:Substituted quinoline-2,4-dicarboxylates (QDCs) are conformationally-restricted mimics of glutamate that were previously reported to selectively block the glutamate vesicular transporters (VGLUTs). We find that expanding the QDC scaffold to benzoquinoline dicarboxylic acids (BQDC) and naphthoquinoline dicarboxylic aci...

journal_title：Bioorganic & medicinal chemistry letters

authors： Carrigan CN,Patel SA,Cox HD,Bolstad ES,Gerdes JM,Smith WE,Bridges RJ,Thompson CM

更新日期：2014-02-01 00:00:00

abstract：:Strontium fructose 1,6-diphosphate (FDP-Sr) is a new strontium-containing compound. The primary aim of this study was to clarify whether the structure component of FDP-Sr, FDP could benefit the protective effect of Sr (II) against oxidative stress induced apoptosis, and meanwhile to further explore the important role ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qi HH,Bao J,Zhang Q,Ma B,Gu GY,Zhang PL,Ou-Yang G,Wu ZM,Ying HJ,Ou-Yang PK

更新日期：2016-10-01 00:00:00

abstract：:We describe here a novel 4-amino-2-cyanopyrimidine scaffold for nonpeptidomimetic cathepsin S selective inhibitors. Some of the synthesized compounds have sub-nanomolar potency and high selectivity toward cathepsin S along with promising pharmacokinetic and physicochemical properties. The key structural features of th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Irie O,Yokokawa F,Ehara T,Iwasaki A,Iwaki Y,Hitomi Y,Konishi K,Kishida M,Toyao A,Masuya K,Gunji H,Sakaki J,Iwasaki G,Hirao H,Kanazawa T,Tanabe K,Kosaka T,Hart TW,Hallett A

更新日期：2008-08-15 00:00:00

abstract：:Sixteen new and one known unsymmetrical open-chain diacylamines were synthesized by sodium methoxide catalyzed acylation of amides with carboxylic esters and acylamino-carboxylic esters, or acylureas with acylamino-carboxylic esters and alpha-amino acid esters. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Weisz I,Roboz J,Wolf I,Szabo J,Bekesi JG

更新日期：1998-11-17 00:00:00

abstract：:Multidrug resistance in tumor cells poses a major obstacle to efficient chemotherapy. Several types of agents have been recognized as multidrug resistance inhibitors, among which the tetrahydroisoquinolines is the most studied. In current study 16 furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinol...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zou ZH,Lan XB,Qian H,Huang WL,Li YM

更新日期：2011-10-01 00:00:00

abstract：:We report (a) on the synthesis of a long-wavelength fluorescent coumarin containing an allyloxy acetate moiety, (b) the synthesis of two linkers containing an allyloxy acetate and an alkyne or azide function, respectively, and (c) the selective modification human serum albumin by a sequential method involving Pd(II) c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cserép GB,Herner A,Wolfbeis OS,Kele P

更新日期：2013-11-01 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：:We have developed a new methodology for producing new molecules that bind to dsDNA using DNA-templated click chemistry. The click reactions between the minor groove binding peptide and acridine intercalators were accelerated by the addition of dsDNA. Furthermore, the resulting peptide-acridine conjugate showed a sligh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Imoto S,Hirohama T,Nagatsugi F

更新日期：2008-10-15 00:00:00

abstract：:Retinoid X Receptor (RXR) specific ligands are currently being investigated for the treatment of metabolic diseases such as type II diabetes. We report the synthesis of conformationally locked retinoids, which are potent RXR selective ligands, and the attempted synthesis of 9-cyclopropyl locked analogs of RA and 9-cis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vuligonda V,Garst ME,Chandraratna RA

更新日期：1999-02-22 00:00:00

abstract：:Novel derivatives of the D-glucosidase inhibitor 2,5-dideoxy-2,5-imino-D-mannitol bearing lipophilic aliphatic or aromatic amides attached to C-1 have been found to inhibit beta-glucosidase from Agrobacterium sp. in the nanomolar range. One of them, a coumarin derivative, ranks amongst the most active compounds in the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wrodnigg TM,Withers SG,Stütz AE

更新日期：2001-04-23 00:00:00

abstract：:Metabolic oligosaccharide engineering is a powerful approach for installing unnatural glycans with unique functional groups into the glycocalyx of living cells and animals. Using this approach, we showed that K(+) channel complexes decorated with thiol-containing sialic acids were irreversibly inhibited with scorpion ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hua Z,Lvov A,Morin TJ,Kobertz WR

更新日期：2011-09-01 00:00:00

abstract：:A series of isoquinuclidine benzamides as glycine uptake inhibitors for the treatment of schizophrenia are described. Potency, lipophilicity, and intrinsic human microsomal clearance were parameters for optimization. Potency correlated with the nature of the ortho substituents of the benzamide ring, and reductions in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Varnes JG,Xiong H,Forst JM,Holmquist CR,Ernst GE,Frietze W,Dembofsky B,Andisik DW,Palmer WE,Hinkley L,Steelman GB,Wilkins DE,Tian G,Jonak G,Potts WM,Wang X,Brugel TA,Alhambra C,Wood MW,Veale CA,Albert JS

更新日期：2018-04-01 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：:The synthesis of six α,β,-unsaturated amides and six 2,4-disubstituted oxazolines derivatives and their evaluation against two Mycobacterium tuberculosis strains (sensitive H37Rv and a resistant clinical isolate) is reported. 2,4-Disubstituted oxazolines (S)-3b,d,e were the most active in the sensitive strain with a M...

journal_title：Bioorganic & medicinal chemistry letters

authors： Avalos-Alanís FG,Hernández-Fernández E,Carranza-Rosales P,López-Cortina S,Hernández-Fernández J,Ordóñez M,Guzmán-Delgado NE,Morales-Vargas A,Velázquez-Moreno VM,Santiago-Mauricio MG

更新日期：2017-02-15 00:00:00

abstract：:A series of 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues were synthesized and evaluated for cytotoxic activity against eight human cancer cell lines. Compounds 18, 21, 28, 29, 30 and 31 showed cytotoxic activity with GI(50) values in the range of 2.1-8.1 microM concentration. Among these, compounds 21...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharma VM,Adi Seshu KV,Vamsee Krishna C,Prasanna P,Chandra Sekhar V,Venkateswarlu A,Rajagopal S,Ajaykumar R,Deevi DS,Rao Mamidi NV,Rajagopalan R

更新日期：2003-05-19 00:00:00

abstract：:Novel benzo[b]thiophene diamine thrombin inhibitors were investigated, focusing on a contracted C4'-side chain series. SAR studies identified compounds with either a pyrrolidino or morpholino group as potent, active site directed thrombin inhibitors when the amino group was connected to the C3-phenyl ring with a methy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takeuchi K,Kohn TJ,Harper RW,Lin HS,Gifford-Moore DS,Richett ME,Sall DJ,Smith GF,Zhang M

更新日期：2000-06-05 00:00:00

abstract：:A prodrug based on a known antibacterial compound is reported to target Staphylococcus aureus and Escherichia coli under reductive conditions. The prodrug was prepared by masking the N-terminus and side chain amines of a component lysine residue as 4-nitrobenzyl carbamates. Activation to liberate the antibacterial was...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yeoh YQ,Horsley JR,Polyak SW,Abell AD

更新日期：2020-06-01 00:00:00

abstract：:Betulinic acid and analogous naturally occurring triterpenoid acids were transformed into the corresponding propargyl esters and subsequently deployed as substrates for a click chemistry-mediated coupling with azidothymidine (AZT) en route to novel 1,2,3-triazole-tethered triterpenoid-AZT conjugates. Twelve new hybrid...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dang Thi TA,Kim Tuyet NT,Pham The C,Thanh Nguyen H,Ba Thi C,Doan Duy T,D'hooghe M,Van Nguyen T

更新日期：2014-11-15 00:00:00

abstract：:The search for new antimicrobial agents is greater than ever due to the perpetual threat of multidrug resistance in known pathogens and the relentless emergence of new infections. In this manuscript, ten thiazole-based thiazolidinone hybrids bearing a 6-trifluoromethoxy substituent on the benzothiazole core were synth...

journal_title：Bioorganic & medicinal chemistry letters

authors： Haroun M,Tratrat C,Petrou A,Geronikaki A,Ivanov M,Ciric A,Sokovic M

更新日期：2021-01-15 00:00:00

abstract：:A series of (R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives (2) have been prepared using parallel synthesis, and their structure-activity relationship studied. High affinity human 5-HT(1B/1D) (h5-HT(1B/1D)) ligands have been identified. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Egle I,MacLean N,Demchyshyn L,Edwards L,Slassi A,Tehim A

更新日期：2003-10-20 00:00:00

abstract：:Horner-Emmons reaction of 4"-dehydro-5-O-TBDMS-avermectin B(1a) with a variety of phosphorus ylides using LHMDS gave novel 4"-alkylidene avermectin derivatives in high yields. Further modifications led to derivatives bearing diverse functional groups. The new avermectin derivatives showed potent growth inhibitory acti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nagai K,Sunazuka T,Shiomi K,Harder A,Turberg A,Omura S

更新日期：2003-11-17 00:00:00

abstract：:Cyano pyrimidine acetylene and cyano pyrimidine t-amine, which belong to a new chemical class, were prepared and tested for inhibitory activities against cathepsin K and the highly homologous cathepsins L and S. The use of novel chemotypes in the development of cathepsin K inhibitors has been demonstrated by derivativ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Teno N,Irie O,Miyake T,Gohda K,Horiuchi M,Tada S,Nonomura K,Kometani M,Iwasaki G,Betschart C

更新日期：2008-04-15 00:00:00

abstract：:Structure-activity relationship (SAR) studies of novel 5-alkyl and 5-aryl/heteroaryl substituted 1,2,4-triazoles are described. The in vitro activity is compared to the pyrazole class of compounds with analogous side chains to delineate the contribution of the triazole ring nitrogen in binding to the active site. Both...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sakya SM,Shavnya A,Cheng H,Li C,Rast B,Li J,Koss DA,Jaynes BH,Mann DW,Petras CF,Seibel SB,Haven ML,Lynch MP

更新日期：2008-02-01 00:00:00

abstract：:Aryl hydroxylamine derivatives have been synthesised that are some of the most potent inhibitors of hCMV protease prepared to date (IC50 14-60 nM). Mass spectrometry studies indicate that oxazinone derived hydroxylamines inhibit the enzyme by acylation of Ser132 whereas non-oxazinone derived hydroxylamines appear to i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Smith DG,Gribble AD,Haigh D,Ife RJ,Lavery P,Skett P,Slingsby BP,Stacey R,Ward RW,West A

更新日期：1999-11-01 00:00:00

abstract：:SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC(50) value of 34 nM. [(11)C]SB-216763 (3-(2,4-dichlorophenyl)-4-(1-[(11)C]methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione), a new potential PET agent for imaging of GSK-3, was first designed and synthesized in 20-30% decay cor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang M,Gao M,Miller KD,Sledge GW,Hutchins GD,Zheng QH

更新日期：2011-01-01 00:00:00