A Dual Reporter Iodinated Labeling Reagent for Cancer Positron Emission Tomography Imaging and Fluorescence-Guided Surgery.

abstract：:The synthesis, biological evaluation, and structure-activity relationships of a series of N-phenyl heteroaryl-fused isothiazolones are described. These isothiazolones have been shown to exhibit potent, dose-dependent inhibition of IL-1 beta-induced breakdown of proteoglycan in a cartilage organ culture assay. This eff...

journal_title：Journal of medicinal chemistry

authors： Wright SW,Petraitis JJ,Abelman MM,Batt DG,Bostrom LL,Corbett RL,Decicco CP,Di Meo SV,Freimark B,Giannaras JV

更新日期：1994-09-16 00:00:00

abstract：:2-Acetamido-5-O-acetyl-6-O-acyl-2-deoxy-3-O-[(R)-2-propionyl-L-alanyl-D- isoglutamine]-D-glucofuranoses, designed as prodrug forms of the corresponding immunoadjuvant-active 6-O-acyl derivatives of N-acetylmuramyl dipeptide (MDP), were synthesized from benzyl 2-acetamido-2-deoxy-5, 6-O-isopropylidene-beta-D-glucofuran...

journal_title：Journal of medicinal chemistry

authors： Durette PL,Dorn CP Jr,Friedman A,Schlabach A

更新日期：1982-09-01 00:00:00

abstract：:In previous studies, we have grouped regions in space occupied by the vitamin D side chain into four: A, G, EA, and EG. We showed that the receptor (VDR) affinity of 1alpha,25-dihydroxyvitamin D3 derivatives increases, in terms of side-chain region, in the order EG, G, A, and EA. We called this the active space group ...

journal_title：Journal of medicinal chemistry

authors： Yamada S,Yamamoto K,Masuno H,Ohta M

更新日期：1998-04-23 00:00:00

abstract：:Structure for the adduct of carbonic anhydrase II with 1-N-(4-sulfamoylphenyl-ethyl)-2,4,6-trimethylpyridinium perchlorate, a membrane-impermeant antitumor sulfonamide, is reported. The phenylethyl moiety fills the active site, making van der Waals interactions with side chains of Gln192, Val121, Phe131, Leu198, Thr20...

journal_title：Journal of medicinal chemistry

authors： Menchise V,De Simone G,Alterio V,Di Fiore A,Pedone C,Scozzafava A,Supuran CT

更新日期：2005-09-08 00:00:00

abstract：:A series of tricyclic indole-2-carboxylic acid derivatives were synthesized and evaluated by the radioligand binding assay and the anticonvulsant effects in the mouse NMDA-induced seizure model. Among them, derivatives of 3S-(-)-4 such as 3a, 3f, and 3g which had certain zwitterionic anilides showed high affinity to t...

journal_title：Journal of medicinal chemistry

authors： Katayama S,Ae N,Kodo T,Masumoto S,Hourai S,Tamamura C,Tanaka H,Nagata R

更新日期：2003-02-27 00:00:00

abstract：:Because of the ambiguities of how to treat ionization in empirical equations which relate biological activity to partition coefficient by use of a (log P)2 term, a theoretical approach to the problem is proposed. Based on a simplified view of assays of potency following in vitro or continuous infusion administration o...

journal_title：Journal of medicinal chemistry

authors： Martin YC,Hackbarth JJ

更新日期：1976-08-01 00:00:00

abstract：:The reaction of platinum salts with bis(naphthalimide), compound 1, yielded two Pt-bis(naphthalimide) complexes, compounds 2 and 3 which differ from each other in their leaving groups being 1,1-cyclobutane dicarboxylate or chloride, respectively. The testing of the cytotoxic activity of compounds 2 and 3 against sever...

journal_title：Journal of medicinal chemistry

authors： Pérez JM,López-Solera I,Montero EI,Brana MF,Alonso C,Robinson SP,Navarro-Ranninger C

更新日期：1999-12-30 00:00:00

abstract：:A series of novel CCK tetrapeptide analogues of the general formula Boc-Trp-Lys(Tac)-N(R)-(CH2)nCON(R')Phe-NH2 (Tac = o-tolylaminocarbonyl), where R,R' = H or Me and n = 1-5, have been synthesized and tested. These analogues, which lack an acidic residue at the penultimate position, demonstrated surprisingly high CCK-...

journal_title：Journal of medicinal chemistry

authors： Elliott RL,Kopecka H,Tufano MD,Shue YK,Gauri AJ,Lin CW,Bianchi BR,Miller TR,Witte DG,Stashko MA

更新日期：1994-05-27 00:00:00

abstract：:Multivalent ligands are promising pharmacological tools that may be more efficacious for several diseases than highly selective single-target drugs. A combined therapy using dopaminergic agonists and adenosinergic antagonists is currently being evaluated for the treatment of Parkinson's disease. [(a) Kanda, T.; et al....

journal_title：Journal of medicinal chemistry

authors： Vendrell M,Angulo E,Casadó V,Lluis C,Franco R,Albericio F,Royo M

更新日期：2007-06-28 00:00:00

abstract：:The currently accepted mechanism of trioxane antimalarial action involves generation of free radicals within or near susceptible sites probably arising from the production of distonic radical anions. An alternative mechanistic proposal involving the ionic scission of the peroxide group and consequent generation of a c...

journal_title：Journal of medicinal chemistry

authors： Drew MG,Metcalfe J,Dascombe MJ,Ismail FM

更新日期：2006-10-05 00:00:00

abstract：:Agonism of GPR119 is viewed as a potential therapeutic approach for the treatment of type II diabetes and other elements of metabolic syndrome. During progression of a previously disclosed candidate 1 through mice toxicity studies, we observed tonic-clonic convulsions in several mice at high doses. An in vitro hippoca...

journal_title：Journal of medicinal chemistry

authors： Scott JS,Bowker SS,Brocklehurst KJ,Brown HS,Clarke DS,Easter A,Ertan A,Goldberg K,Hudson JA,Kavanagh S,Laber D,Leach AG,MacFaul PA,Martin EA,McKerrecher D,Schofield P,Svensson PH,Teague J

更新日期：2014-11-13 00:00:00

abstract：:A group of peptide-based, long-acting, stable, highly selective cholecystokinin 1 receptor (CCK-1R) agonists with the potential to treat obesity has been identified and characterized, based on systematic investigation of synthetic CCK-8 analogues with N-terminal linkage to fatty acids. Sulfated Tyr in such compounds w...

journal_title：Journal of medicinal chemistry

authors： Sensfuss U,Kruse T,Skyggebjerg RB,Uldam HK,Vestergaard B,Huus K,Vinther TN,Reinau ME,Schéele S,Clausen TR

更新日期：2019-02-14 00:00:00

abstract：:A number of bis(diazeniumdiolates) that we designed to release up to 4 mol of nitric oxide (NO) and that are structural analogues of the NO prodrug and anticancer lead compound O(2)-{2,4-dinitro-5-[4-(N-methylamino)benzoyloxy]phenyl} 1-(N,N-dimethylamino)diazen-1-ium-1,2- diolate (PABA/NO) were synthesized and studied...

journal_title：Journal of medicinal chemistry

authors： Andrei D,Maciag AE,Chakrapani H,Citro ML,Keefer LK,Saavedra JE

更新日期：2008-12-25 00:00:00

abstract：:Protein-protein interfaces provide an important class of drug targets currently receiving increased attention. The typical design strategy to inhibit protein-protein interactions usually involves large molecules such as peptides and macrocycles. One exception is tranexamic acid (TXA), which, as a lysine mimetic, inhib...

journal_title：Journal of medicinal chemistry

authors： Boström J,Grant JA,Fjellström O,Thelin A,Gustafsson D

更新日期：2013-04-25 00:00:00

abstract：:Indoleamine 2,3-dioxygenase 1 (IDO1) catalyzes the rate-limiting step in the kynurenine pathway of tryptophan metabolism, which is involved in immunity, neuronal function, and aging. Its implication in pathologies such as cancer and neurodegenerative diseases has stimulated the development of IDO1 inhibitors. However,...

journal_title：Journal of medicinal chemistry

authors： Röhrig UF,Reynaud A,Majjigapu SR,Vogel P,Pojer F,Zoete V

更新日期：2019-10-10 00:00:00

abstract：:Potent and selective inhibitors of Dyrk1B kinase were developed to explore the hypothesis, based on siRNA studies, that Dyrk1B may be a resistance mechanism in cells undergoing a stress response. ...

journal_title：Journal of medicinal chemistry

authors： Kettle JG,Ballard P,Bardelle C,Cockerill M,Colclough N,Critchlow SE,Debreczeni J,Fairley G,Fillery S,Graham MA,Goodwin L,Guichard S,Hudson K,Ward RA,Whittaker D

更新日期：2015-03-26 00:00:00

abstract：:Protein tyrosine phosphatases (PTPases) are involved in the control of tyrosine phosphorylation levels in the cell and are believed to be crucial for the regulation of a multitude of cellular functions. A detailed understanding of the role played by PTPases in various signaling pathways has not yet been achieved, and ...

journal_title：Journal of medicinal chemistry

authors： Sarmiento M,Wu L,Keng YF,Song L,Luo Z,Huang Z,Wu GZ,Yuan AK,Zhang ZY

更新日期：2000-01-27 00:00:00

abstract：:Nonalcoholic steatohepatitis (NASH) is a severe form of nonalcoholic fatty liver disease (NAFLD) characterized by liver steatosis, inflammation, and hepatocellular damage. NASH is a serious condition that can progress to cirrhosis, liver failure, and hepatocellular carcinoma. The association of NASH with obesity, type...

journal_title：Journal of medicinal chemistry

authors： Romero FA,Jones CT,Xu Y,Fenaux M,Halcomb RL

更新日期：2020-05-28 00:00:00

abstract：:Mutant epidermal growth factor receptor (EGFR) is a major driver of non-small-cell lung cancer (NSCLC). Marketed first generation inhibitors, such as erlotinib, effect a transient beneficial response in EGFR mutant NSCLC patients before resistance mechanisms render these inhibitors ineffective. Secondary oncogenic EGF...

journal_title：Journal of medicinal chemistry

authors： Planken S,Behenna DC,Nair SK,Johnson TO,Nagata A,Almaden C,Bailey S,Ballard TE,Bernier L,Cheng H,Cho-Schultz S,Dalvie D,Deal JG,Dinh DM,Edwards MP,Ferre RA,Gajiwala KS,Hemkens M,Kania RS,Kath JC,Matthews J,Murra

更新日期：2017-04-13 00:00:00

abstract：:The human brain is a uniquely complex organ, which has evolved a sophisticated protection system to prevent injury from external insults and toxins. Designing molecules that can overcome this protection system and achieve optimal concentration at the desired therapeutic target in the brain is a specific and major chal...

journal_title：Journal of medicinal chemistry

authors： Rankovic Z

更新日期：2015-03-26 00:00:00

abstract：:Mercaptopurine (6-MP), thioguanine (6-TG), and azathioprine (AZA) are purine antimetabolites introduced as anticancer or immunosuppressive drugs decades ago. Methylated AZA, called MAZA, is among the investigational drugs. The present study compares MAZA to the widely recognized drugs AZA, 6-MP, and 6-TG with respect ...

journal_title：Journal of medicinal chemistry

authors： Hoffmann M,Chrzanowska M,Hermann T,Rychlewski J

更新日期：2005-06-30 00:00:00

abstract：:The synthesis of a series of 1-phenoxy-3-[[(substituted-amido)alkyl]amino]-2-propanols is described. Many of the compounds are more potent than propanolol as beta blockers, while having cardioselectivity comparable to that of practolol, when given intravenously to anesthetized cats. The structure-activity relationship...

journal_title：Journal of medicinal chemistry

authors： Lare MS,Smith LH

更新日期：1982-11-01 00:00:00

abstract：:This paper describes the chemical synthesis and CCK-B and CCK-A receptor binding affinities of a series of compounds in which the central amide bond of the CCK-B "dipeptoid" ligand tricyclo[3.3.1.1(3,7)]dec-2-yl [R-(R*,S*)]-[2-[[1-(hydroxymethyl)- 2-phenylethyl]amino]-1-(1H-indol-3-ylmethyl)-2-oxoethyl]carb amate (4) ...

journal_title：Journal of medicinal chemistry

authors： Fincham CI,Higginbottom M,Hill DR,Horwell DC,O'Toole JC,Ratcliffe GS,Rees DC,Roberts E

更新日期：1992-04-17 00:00:00

abstract：:KEAP1 is the key regulator of the NRF2-mediated cytoprotective response, and increasingly recognized as a target for diseases involving oxidative stress. Pharmacological intervention has focused on molecules that decrease NRF2-ubiquitination through covalent modification of KEAP1 cysteine residues, but such electrophi...

journal_title：Journal of medicinal chemistry

authors： Davies TG,Wixted WE,Coyle JE,Griffiths-Jones C,Hearn K,McMenamin R,Norton D,Rich SJ,Richardson C,Saxty G,Willems HM,Woolford AJ,Cottom JE,Kou JP,Yonchuk JG,Feldser HG,Sanchez Y,Foley JP,Bolognese BJ,Logan G,Podoli

更新日期：2016-04-28 00:00:00

abstract：:Selective inhibitors of the two paralogue KAT3 acetyltransferases (CBP and p300) may serve not only as precious chemical tools to investigate the role of these enzymes in physiopathological mechanisms but also as lead structures for the development of further antitumor agents. After the application of a molecular prun...

journal_title：Journal of medicinal chemistry

authors： Milite C,Feoli A,Sasaki K,La Pietra V,Balzano AL,Marinelli L,Mai A,Novellino E,Castellano S,Tosco A,Sbardella G

更新日期：2015-03-26 00:00:00

abstract：:3',5'-Cyclic adenosine monophosphate (cAMP) is a pivotal second messenger that regulates numerous biological processes under physiological and pathological conditions, including cancer, diabetes, heart failure, inflammation, and neurological disorders. In the past, all effects of cAMP were initially believed to be med...

journal_title：Journal of medicinal chemistry

authors： Chen H,Wild C,Zhou X,Ye N,Cheng X,Zhou J

更新日期：2014-05-08 00:00:00

abstract：:The medicinal chemistry community has directed considerable efforts toward the discovery of selective inhibitors of interleukin-2 inducible T-cell kinase (ITK), given its role in T-cell signaling downstream of the T-cell receptor (TCR) and the implications of this target for inflammatory disorders such as asthma. We h...

journal_title：Journal of medicinal chemistry

authors： Burch JD,Barrett K,Chen Y,DeVoss J,Eigenbrot C,Goldsmith R,Ismaili MH,Lau K,Lin Z,Ortwine DF,Zarrin AA,McEwan PA,Barker JJ,Ellebrandt C,Kordt D,Stein DB,Wang X,Chen Y,Hu B,Xu X,Yuen PW,Zhang Y,Pei Z

更新日期：2015-05-14 00:00:00

abstract：:In a previous paper, we reported the N-hydroxyformamidine derivative HET0016 as a potent and selective 20-HETE synthase inhibitor. Despite its attraction as a potential therapeutic agent for cerebral diseases, the preparation of an injectable formulation of HET0016 was limited by its poor solubility under neutral cond...

journal_title：Journal of medicinal chemistry

authors： Nakamura T,Sato M,Kakinuma H,Miyata N,Taniguchi K,Bando K,Koda A,Kameo K

更新日期：2003-12-04 00:00:00

abstract：:Following erythrocyte invasion, malaria parasites export a catalogue of remodeling proteins into the infected cell that enable parasite development in the human host. Export is dependent on the activity of the aspartyl protease, plasmepsin V (PMV), which cleaves proteins within the Plasmodium export element (PEXEL; Rx...

journal_title：Journal of medicinal chemistry

authors： Sleebs BE,Gazdik M,O'Neill MT,Rajasekaran P,Lopaticki S,Lackovic K,Lowes K,Smith BJ,Cowman AF,Boddey JA

更新日期：2014-09-25 00:00:00

abstract：:omega-Acryloyl anionic surfactants, whose polar heads are derived from amino acids, have been telomerized to prepare polyanions of a predetermined molecular weight. The main goal of this study was to verify whether the antiviral activity is influenced by the degree of polymerization of the polyanions. The oligomeric p...

journal_title：Journal of medicinal chemistry

authors： Leydet A,Barragan V,Boyer B,Montéro JL,Roque JP,Witvrouw M,Este J,Snoeck R,Andrei G,De Clercq E

更新日期：1997-01-31 00:00:00