Polycyclic aromatic compounds as anticancer agents: synthesis and biological evaluation of some chrysene derivatives.

abstract：:2-O-carboxymethylpyrogallol derivatives (4-17) were synthesized, with their in vitro inhibitory activities against PTP1B and in vivo antihyperglycemic effects examined. Compound 14, the most potent among the series, showed a K(i) value of 1.1 microM against PTP1B, 7-fold lower than that against TC-PTP. When compound 1...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhattarai BR,Shrestha S,Ham SW,Kim KR,Cheon HG,Lee KH,Cho H

更新日期：2007-10-01 00:00:00

abstract：:The reactivity of 4-[13C]- and 5-[13C]-5-chloro-2-methylisothiazol-3-one (MCI) and 2-methylisothiazol-3-one (MI) towards a model peptide and glutathione was followed by 13C and 1H[13C] NMR spectroscopy. Both molecules were found to react with GSH but in addition MCI was found to react with histidine and lysine to form...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alvarez-Sánchez R,Basketter D,Pease C,Lepoittevin JP

更新日期：2004-01-19 00:00:00

abstract：:Inositols play an important role in membrane lipid metabolism and mitogenic signaling of most cancer cells. There is paucity of data on the distribution of radiolabelled inositols. Based on work previously carried out on 1-deoxy-1-[(18)F]fluoro-scyllo-inositol ([(18)F]2), we began a program of work to label myo-inosit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Carroll L,Perumal M,Vasdev N,Robins E,Aboagye EO

更新日期：2012-10-01 00:00:00

abstract：:Corticotropin-releasing factor (CRF), a 41 amino acid peptide neurohormone synthesised by specific hypothalamic nuclei in the brain, is implicated in stress-related function. Antagonism of CRF(1) receptors is an attractive therapeutic approach for the treatment of depression and anxiety. Unsaturated tetrahydrotriazaac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gentile G,Di Fabio R,Pavone F,Sabbatini FM,St-Denis Y,Zampori MG,Vitulli G,Worby A

更新日期：2007-09-15 00:00:00

abstract：:A series of N-(1-methyl-1H-indol-3-yl)methyleneamines and eight new 3,3-diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized and screened for their antileishmanial activity against Leishmania major. 3,3-Diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized by the Staudinger's ketene-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh GS,Al-Kahraman YM,Mpadi D,Yasinzai M

更新日期：2012-09-01 00:00:00

abstract：:A novel series of compounds derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one) is described. Extensive SAR studies resulted in compounds with IC(50) values in the range of 10-150 nM and selectivity over the L-type channels up to nearly...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pajouhesh H,Feng ZP,Ding Y,Zhang L,Pajouhesh H,Morrison JL,Belardetti F,Tringham E,Simonson E,Vanderah TW,Porreca F,Zamponi GW,Mitscher LA,Snutch TP

更新日期：2010-02-15 00:00:00

abstract：:We have optimized 2-aminomethylphenylamine derivative as a factor Xa inhibitor. Several polar functional groups were introduced in the central phenyl ring, and we focused on zwitter ionic compound showing continuous inhibitory activity in oral administration test. In vitro and oral activities were improved by optimiza...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mochizuki A,Nagata T,Kanno H,Takano D,Kishida M,Suzuki M,Ohta T

更新日期：2011-12-15 00:00:00

abstract：:The Van enzymes are ATP-dependant ligases responsible for resistance to vancomycin in Staphylococcus aureus and Enteroccoccus species. The de novo molecular design programme SPROUT was used in conjunction with the X-ray crystal structure of Enterococcus faeciumd-alanyl-d-lactate ligase (VanA) to design new putative in...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sova M,Cadez G,Turk S,Majce V,Polanc S,Batson S,Lloyd AJ,Roper DI,Fishwick CW,Gobec S

更新日期：2009-03-01 00:00:00

abstract：:The alpha7 subtype of the nicotinic acetylcholine receptor (nAChR) is the target of studies aimed at identifying features that will lead to the development of selective therapeutics. Five arylidine anabaseines, three with pyridine rings and two with the pyrrole rings, were synthesized in 35-65% yield via aldol condens...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang J,Papke RL,Horenstein NA

更新日期：2009-01-15 00:00:00

abstract：:A serendipitous discovery that the metalloprotease binding profile of a novel class of 2-carboxamide-3-hydroxamic acid piperidines could be significantly attenuated by the modification of the unexplored P1 substituent enabled the design and synthesis of a novel 2-carboxamide-1-hydroxamic acid cyclohexyl scaffold core ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Burns DM,Li YL,Shi E,He C,Xu M,Zhuo J,Zhang C,Qian DQ,Li Y,Wynn R,Covington MB,Katiyar K,Marando CA,Fridman JS,Scherle P,Friedman S,Metcalf B,Yao W

更新日期：2009-07-01 00:00:00

abstract：:A small set of 9-aminoacridine-3- and 4-carboxamides were synthesized efficiently using the benzyne/azide click chemistry. The products bind to duplex DNA but have different antitumour activity in the HL60 cell line. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Howell LA,Howman A,O'Connell MA,Mueller A,Searcey M

更新日期：2009-10-15 00:00:00

abstract：:Two new technetium complexes containing a piperidine template have been synthesized and evaluated as possible leads for the development of dopamine transporter (DAT) imaging agents. Binding data for the corresponding rhenium complexes containing either a monoaminomonoamide (MAMA') or a diaminodithiol (DADT) chelating ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hoepping A,Babich J,Zubieta JA,Johnson KM,Machill S,Kozikowski AP

更新日期：1999-11-15 00:00:00

abstract：:The design, synthesis, and biological evaluation of arylsulfonamidooxazoles as 11beta-HSD1 inhibitors and the serendipitous discovery of beta-keto sulfones as potent 11beta-HSD1 inhibitors are described here. These two classes of compounds are not active against 11beta-HSD2 and therefore may have significant therapeut...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiang J,Ipek M,Suri V,Massefski W,Pan N,Ge Y,Tam M,Xing Y,Tobin JF,Xu X,Tam S

更新日期：2005-06-02 00:00:00

abstract：:A quantitative structure-activity relationship (QSAR) modeling of the antimold activity of cinnamaldehyde analogues against of Aspergillus niger and Paecilomyces variotii was presented. The molecular descriptors of cinnamaldehyde analogues were calculated by the CODESSA program, and these descriptors were selected by ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Y,Li S,Kong X

更新日期：2013-03-01 00:00:00

abstract：:Two new merosesquiterpenes, verruculides A (1) and B (2), were isolated from a culture broth of the Indonesian ascidian-derived Penicillium verruculosum TPU1311, together with three known congeners, chrodrimanins A (3), B (4), and H (5). The structures of 1 and 2 were assigned on the basis of their spectroscopic data ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yamazaki H,Nakayama W,Takahashi O,Kirikoshi R,Izumikawa Y,Iwasaki K,Toraiwa K,Ukai K,Rotinsulu H,Wewengkang DS,Sumilat DA,Mangindaan RE,Namikoshi M

更新日期：2015-08-15 00:00:00

abstract：:A methyl group at the 2-position of methyl mesopyropheophorbide-a was transformed to the 2-formyl group to give methyl mesopyropheophorbide-f, one of the chlorophyll-f analogs. The 2-formylation moved the redmost electronic absorption band in a solution to a longer wavelength and the bathochromic shift was comparable ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu M,Kinoshita Y,Tamiaki H

更新日期：2014-08-15 00:00:00

abstract：:The in vitro evaluation of a series of saturated prostaglandins revealed that compounds with omega chain aromatic rings retain nanomolar potency for the human prostaglandin F receptor (hFP receptor), exemplified by compound 8. In contrast, the double bonds are required for activity in the series with an acyclic omega ...

journal_title：Bioorganic & medicinal chemistry letters

authors： deLong MA,Amburgey J,Taylor C,Wos JA,Soper DL,Wang Y,Hicks R

更新日期：2000-07-17 00:00:00

abstract：:A series of COX-2 selective inhibitor nimesulide derivatives were synthesized. Their anti-cell proliferation activities were evaluated with a long-term estrogen deprived MCF-7aro (LTEDaro) breast cancer cell line, which is the biological model of aromatase inhibitor resistance for hormone-dependent breast cancer. Comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Su B,Chen S

更新日期：2009-12-01 00:00:00

abstract：:Prostate-specific membrane antigen (PSMA) is an important biological target for therapy and diagnosis of prostate cancer. In this study, novel multivalent PSMA inhibitors with glutamate-urea-lysine structures were designed to improve inhibition characteristics. Precursors of the novel inhibitors were prepared from glu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kwon YD,Chung HJ,Lee SJ,Lee SH,Jeong BH,Kim HK

更新日期：2018-02-15 00:00:00

abstract：:The Gram-negative bacterium Acinetobacter baumannii is an opportunistic pathogen in humans and infections are poorly treated by current therapy. Recent emergence of multi-drug resistant strains and the lack of new antibiotics demand an immediate action for development of new anti-Acinetobacter agents. To this end, oxi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rubin H,Selwood T,Yano T,Weaver DG,Loughran HM,Costanzo MJ,Scott RW,Wrobel JE,Freeman KB,Reitz AB

更新日期：2015-01-15 00:00:00

abstract：:Ligand-based virtual screening led to the discovery of a new class of potent inverse agonists of the human cannabinoid receptor 1, hCB(1), which are selective versus hCB(2). These CB(1) ligands present intriguing departures from a classical CB(1) antagonist pharmacophore. Elements of SAR are discussed in this context....

journal_title：Bioorganic & medicinal chemistry letters

authors： Foloppe N,Allen NH,Bentley CH,Brooks TD,Kennett G,Knight AR,Leonardi S,Misra A,Monck NJ,Sellwood DM

更新日期：2008-02-01 00:00:00

abstract：:A new class of potent NK3R antagonists based on the N',2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ(90) 30 mg/kg po; plasma Occ(90) 0.95 microM) and has good selectivity and promising PK properti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Elliott JM,Carling RW,Chambers M,Chicchi GG,Hutson PH,Jones AB,MacLeod A,Marwood R,Meneses-Lorente G,Mezzogori E,Murray F,Rigby M,Royo I,Russell MG,Sohal B,Tsao KL,Williams B

更新日期：2006-11-15 00:00:00

abstract：:Scaffold hybridization of several natural and synthetic anticancer leads led to the consideration of indenoindolones as potential novel anticancer agents. A series of these compounds were prepared by a diversity-feasible synthetic method. They were found to possess anticancer activities with higher potency compared to...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kashyap M,Das D,Preet R,Mohapatra P,Satapathy SR,Siddharth S,Kundu CN,Guchhait SK

更新日期：2012-04-01 00:00:00

abstract：:Constraining the catechol aryl ether moiety of bastadins by incorporation into a macrocyle is not necessary in order to mimic the effects of these marine natural products on neuronal calcium homeostasis. Simple, acyclic analogs that embody the 'western' or 'eastern' parts of bastadins were found to evoke comparable re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zieminska E,Lazarewicz JW,Couladouros EA,Moutsos VI,Pitsinos EN

更新日期：2008-11-01 00:00:00

abstract：:Glycosyldisulfides can interact efficiently with carbohydrate-binding entities. This has been shown for a range of thiosaccharide dimers when tested for their effects against the lectin Concanavalin A using a modified quartz crystal microbalance-technique. Contrary to the thiosaccharide monomers, showing no significan...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pei Z,Aastrup T,Anderson H,Ramström O

更新日期：2005-06-02 00:00:00

abstract：:Two new C(29) sterols with a cyclopropane ring at C-25 and C-26, petrosterol-3,6-dione (1) and 5alpha,6alpha-epoxy-petrosterol (2), along with petrosterol (3), were isolated from the Vietnamese marine sponge Ianthella sp. The structures of the new compounds were elucidated by comprehensive spectroscopic analyses. Comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen HT,Chau VM,Tran TH,Phan VK,Hoang TH,Nguyen TD,Nguyen XN,Tai BH,Hyun JH,Kang HK,Kim YH

更新日期：2009-08-15 00:00:00

abstract：:A series of imidazolopyrazinones 3, substituted at C-2, and C-2/C-6, has been prepared. The compounds behaved as quenchers of superoxide anion. The more active compounds are structurally related to coelenterazine, a natural substrate of marine bioluminescence. Theoretical parameters based on Hartree-Fock instabilities...

journal_title：Bioorganic & medicinal chemistry letters

authors： Devillers I,Dive G,De Tollenaere C,Falmagne B,de Wergifosse B,Rees JF,Marchand-Brynaert J

更新日期：2001-09-03 00:00:00

abstract：:Anions represent the second class of inhibitors of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), in addition to sulfonamides, which possess clinical applications. The first inhibition study of the zinc and cobalt gamma-class enzyme from the archaeon Methanosarcina thermophila (Cam) with anions is reported here....

journal_title：Bioorganic & medicinal chemistry letters

authors： Innocenti A,Zimmerman S,Ferry JG,Scozzafava A,Supuran CT

更新日期：2004-06-21 00:00:00

abstract：:The synthesis and biological activity of sordarin oxazepine derivatives are described. The key step features a regioselective oxidation of an unprotected triol followed by double reductive amination to afford the ring-closed products. The spectrum of antifungal activity for these novel derivatives includes coverage of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Serrano-Wu MH,St Laurent DR,Chen Y,Huang S,Lam KR,Matson JA,Mazzucco CE,Stickle TM,Tully TP,Wong HS,Vyas DM,Balasubramanian BN

更新日期：2002-10-07 00:00:00

abstract：:Bromodomains (BRDs) recognize acetyl-lysine modified histone tails mediating epigenetic processes. BRD4, a protein containing two bromodomains, has emerged as an attractive therapeutic target for several types of cancer as well as inflammatory diseases. Using a fragment-based in silico screening approach, we identifie...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao H,Gartenmann L,Dong J,Spiliotopoulos D,Caflisch A

更新日期：2014-06-01 00:00:00