Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.

abstract：:A series of novel pyrimido[1,2-b]indazoles 5, 7 have been prepared from 3-trifluoromethyl-5-phenyl-2,6-dicyano anilines 1 via novel indazole regioisomers 3 and 4 through a facile strategy. Specific examples were evaluated for anticancer activity in vitro and found to exhibit promising activity against A-549 cell lines...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yakaiah T,Lingaiah BP,Narsaiah B,Shireesha B,Ashok Kumar B,Gururaj S,Parthasarathy T,Sridhar B

更新日期：2007-06-15 00:00:00

abstract：:In this study, 5-methylmellein (5-MM) loaded bovine serum albumin nanoparticles (BSA NPs) were developed using desolvation technique. The developed nanoparticles were characterized for their mean particle size, polydispersity, zeta potential, loading efficiency, X-ray diffractometry (XRD), differential scanning calori...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arora D,Kumar A,Gupta P,Chashoo G,Jaglan S

更新日期：2017-12-01 00:00:00

abstract：:A general protocol for the synthesis of paclitaxel C-10 carbamates is described. The method entails MeI-mediated activation of 2'-O-TBS-7-O-TES-10-O-deacetyl-paclitaxel-10-O-carbonylimidazole prior to reaction with amines. This method is effective for the synthesis of paclitaxel C-10 derivatives, including bifunctiona...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ballatore C,Aspland SE,Castillo R,Desharnais J,Eustaquio T,Sun C,Castellino AJ,Smith AB 3rd

更新日期：2005-05-16 00:00:00

abstract：:The transporter protein Large-neutral Amino Acid Transporter 1 (LAT-1, SLC7A5) is responsible for transporting amino acids such as tyrosine and phenylalanine as well as thyroid hormones, and it has been exploited as a drug delivery mechanism. Recently its role in cancer has become increasingly appreciated, as it has b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Augustyn E,Finke K,Zur AA,Hansen L,Heeren N,Chien HC,Lin L,Giacomini KM,Colas C,Schlessinger A,Thomas AA

更新日期：2016-06-01 00:00:00

abstract：:We herein report a group of allosteric inhibitors of integrin alpha(2)beta(1) based on an arylamide scaffold. Compound 4 showed an IC(50) of 4.80 microM in disrupting integrin I-domain/collagen binding in an ELISA. These arylamide compounds are able to block collagen binding to integrin alpha(2)beta(1) on the platelet...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yin H,Gerlach LO,Miller MW,Moore DT,Liu D,Vilaire G,Bennett JS,DeGrado WF

更新日期：2006-07-01 00:00:00

abstract：:Pyridone-based peptidomimetic inhibitors of recombinant human Interleukin-1 beta-converting enzyme (ICE, caspase-1) with an aminomethylene ketone activating group in the P1' position are described. Several analogues with sub-nanomolar Ki's versus ICE and improved aqueous solubility are reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Semple G,Ashworth DM,Batt AR,Baxter AJ,Benzies DW,Elliot LH,Evans DM,Franklin RJ,Hudson P,Jenkins PD,Pitt GR,Rooker DP,Yamamoto S,Isomura Y

更新日期：1998-04-21 00:00:00

abstract：:The impact of lipophilicity as a factor contributing to hERG potency is assessed for a large dataset of compounds of differing ionisation type. This dataset is derived from compounds tested in the IonWorks-based in vitro electrophysiology hERG assay at AstraZeneca. Using logistic regression, a quantification of the ri...

journal_title：Bioorganic & medicinal chemistry letters

authors： Waring MJ,Johnstone C

更新日期：2007-03-15 00:00:00

abstract：:Paclitaxel (PTX) was complexed with beta-cyclodextrin (1), 2,6-dimethyl-beta-cyclodextrin (2) and 2,3,6-trimethyl-beta-cyclodextrin (3). PTX-CYD complexes were characterized both at the solid and liquid states. Experimental findings are in agreement with molecular modeling analysis, which showed different PTX-CYD inte...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alcaro S,Ventura CA,Paolino D,Battaglia D,Ortuso F,Cattel L,Puglisi G,Fresta M

更新日期：2002-06-17 00:00:00

abstract：:A novel alpha7 nAChR agonist, N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (3a, PHA-709829), has been identified for the potential treatment of cognitive deficits in schizophrenia. The compound shows potent and selective alpha7 in vitro activity, excellent brain penetration, good rat oral b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Acker BA,Jacobsen EJ,Rogers BN,Wishka DG,Reitz SC,Piotrowski DW,Myers JK,Wolfe ML,Groppi VE,Thornburgh BA,Tinholt PM,Walters RR,Olson BA,Fitzgerald L,Staton BA,Raub TJ,Krause M,Li KS,Hoffmann WE,Hajos M,Hurst RS,

更新日期：2008-06-15 00:00:00

abstract：:A water-soluble derivative of N-fused porphyrin (NFP) possessing a nona-arginine (R9) peptide tail was synthesized for the first time by a Cu(I)-catalyzed azide-alkyne 'click' reaction. In aqueous solution, at pH 8, the conjugated molecule (NFP-R9) exists as free base and protonated below pH<6.5 to form monoprotonated...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ikawa Y,Harada H,Toganoh M,Furuta H

更新日期：2009-05-01 00:00:00

abstract：:A series of indole ring containing compounds were designed based on the structure of the gp41 complex in the region of the hydrophobic pocket. These compounds were synthesized using a Suzuki Coupling reaction, and evaluated using a fluorescence binding assay and cell-cell fusion assay. The observed inhibition constant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhou G,Wu D,Hermel E,Balogh E,Gochin M

更新日期：2010-03-01 00:00:00

abstract：:The relaxin family peptide receptors have been implicated in numerous physiological processes including energy homeostasis, cardiac function, wound healing, and reproductive function. Two family members, RXFP3 and RXFP4, are class A GPCRs with endogenous peptide ligands (relaxin-3 and insulin-like peptide 5 (INSL5), r...

journal_title：Bioorganic & medicinal chemistry letters

authors： DeChristopher B,Park SH,Vong L,Bamford D,Cho HH,Duvadie R,Fedolak A,Hogan C,Honda T,Pandey P,Rozhitskaya O,Su L,Tomlinson E,Wallace I

更新日期：2019-04-15 00:00:00

abstract：: ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng JH,Hu XL,Lv XY,Wang BL,Lin J,Zhang XQ,Ye WC,Xiong F,Wang H

更新日期：2019-01-15 00:00:00

abstract：:Screening of the Maybridge compound collection identified 4-arylphthalazinones as micromolar inhibitors of PARP-1 catalytic activity. Subsequent optimisation of both inhibitory activity and metabolic stability led to a novel series of meta-substituted 4-benzyl-2H-phthalazin-1-ones with low nanomolar, cellular activity...

journal_title：Bioorganic & medicinal chemistry letters

authors： Loh VM Jr,Cockcroft XL,Dillon KJ,Dixon L,Drzewiecki J,Eversley PJ,Gomez S,Hoare J,Kerrigan F,Matthews IT,Menear KA,Martin NM,Newton RF,Paul J,Smith GC,Vile J,Whittle AJ

更新日期：2005-05-02 00:00:00

abstract：:Following the discovery of N-acyl-1,4-diazepan-2-one as a novel pharmacophore for potent and selective DPP-4 inhibitors, optimization of this new lead with different substitution on the seven-membered ring resulted in several highly potent and selective, orally bioavailable, and efficacious DPP-4 inhibitors, such as 3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liang GB,Qian X,Feng D,Biftu T,Eiermann G,He H,Leiting B,Lyons K,Petrov A,Sinha-Roy R,Zhang B,Wu J,Zhang X,Thornberry NA,Weber AE

更新日期：2007-04-01 00:00:00

abstract：:We identified and tested bisphosphonates as inhibitors of a protozoan molecular target. Computational modeling studies demonstrated that these compounds are mimics of the natural substrate of the enzyme. The most potent bisphosphonates in vitro are pamidronate and risedronate, which inhibit the purine transferase from...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fernández D,Wenck MA,Craig SP 3rd,Delfino JM

更新日期：2004-09-06 00:00:00

abstract：:Selectivity of enzymatic and chemical methods for transesterifications of cytarabine with divinyl dicarboxylates was described. Catalysis by lipase acrylic resin from Candida antarctica (CAL-B) in acetone facilitated the single step synthesis of polymerizable 5'-O-acyl cytarabine derivatives in high yields, while the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang N,Chen ZC,Lu DS,Lin XF

更新日期：2005-09-15 00:00:00

abstract：:Homooligomers constructed with 4- and 6-amino acid fragments of melanocortin (alpha-MSH) bind with higher affinity and with apparent cooperativity to melanocortin receptor, compared to their constituent monomers. Individual ligands were tethered with various spacers of different length and rigidity and the influence o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vagner J,Handl HL,Gillies RJ,Hruby VJ

更新日期：2004-01-05 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 series of novel 2,3-dihydro-4H-1-benzoselenin-4-one (thio)semicarbazone derivatives were designed and synthesized by using molecular hybridization approach. All the target compounds were characterized by HRMS and NMR and evaluated in vitro antifungal activity against five pathogenic strains. In comparison with precu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu H,Su X,Liu XQ,Zhang KP,Hou Z,Guo C

更新日期：2019-12-01 00:00:00

abstract：:Mannose-6-phosphate (M6P)-containing N-linked glycans are essential signaling molecules for sorting hydrolases in eukaryotic cells. Their receptors, especially the cation-independent M6P receptors (CI-MPRs), have emerged as promising protein targets for targeted drug delivery for the treatment of lysosomal storage dis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu Y,Marshall J,Li Q,Edwards N,Chen G

更新日期：2013-04-15 00:00:00

abstract：:Triphosphate of a new fluorescent labeled thymidine analogue was incorporated as a substrate for PCR using KOD Dash DNA polymerase forming the corresponding fluorescent labeled DNA which is useful for a DNA probe. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Obayashi T,Masud MM,Ozaki AN,Ozaki H,Kuwahara M,Sawai H

更新日期：2002-04-22 00:00:00

abstract：:In this Letter, we report the structure-activity relationship (SAR) studies on series of positional isomers of 5(6)-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles derivatives 7(a-j) and 8(a-j) synthesized in good yields and characterized by (1)H NMR, (13)C NMR and mass spectral analyses. The c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ranjith PK,Rajeesh P,Haridas KR,Susanta NK,Row TN,Rishikesan R,Kumari NS

更新日期：2013-09-15 00:00:00

abstract：:A series of bis(indolyl) hydrazide-hydrazones 5a-n were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-carboxaldehyde 2 with indole-3-carbohydrazide 4 in presence of catalytic amount of acetic acid afforded 5a-n in good yields. Among the synthesized ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumar D,Maruthi Kumar N,Ghosh S,Shah K

更新日期：2012-01-01 00:00:00

abstract：:A number of novel 1-(3-arylprop-2-ynyl) substituted 1,2-dihydroquinoline derivatives related to nimesulide and their 2-oxo analogues have been designed as potential inhibitors of PDE4. All these compounds were synthesized by using Sonogashira coupling as a key step. In vitro PDE4B inhibitory properties and molecular m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pal S,Durgadas S,Nallapati SB,Mukkanti K,Kapavarapu R,Meda CL,Parsa KV,Pal M

更新日期：2011-11-01 00:00:00

abstract：:We sought to design dual pharmacology bronchodilators targeting both the M(3) muscarinic acetylcholine and beta-2 adrenergic (β(2)) receptors by applying our multivalent approach to drug discovery. Herein, we describe our initial discovery and the SAR of the first such compounds with matched potencies at both receptor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hughes AD,Chin KH,Dunham SL,Jasper JR,King KE,Lee TW,Mammen M,Martin J,Steinfeld T

更新日期：2011-03-01 00:00:00

abstract：:New analogues of the previously described 3-aryl pyridone KOR agonists have been synthesised by parallel synthetic methods, both in solution- and with solid-phase chemistry, making use of the well known and versatile Mitsunobu, Suzuki and Buchwald reactions. Opioid receptor binding data for the compounds produced is r...

journal_title：Bioorganic & medicinal chemistry letters

authors： Semple G,Andersson BM,Chhajlani V,Georgsson J,Johansson MJ,Rosenquist A,Swanson L

更新日期：2003-03-24 00:00:00

abstract：:Pholasin is a bioluminescent photoprotein of Pholas dactylus. Pholasin is a commercially available photoprotein used to measure intracellular reactive oxygen species. Although extensive efforts have been carried out to determine the chemical structure of the prosthetic (chromophore) group, it still remains unclear to ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kuse M,Tanaka E,Nishikawa T

更新日期：2008-10-15 00:00:00

abstract：:We have synthesized a novel vitamin D receptor agonist VS-105 ((1R,3R)-5-((E)-2-((3αS,7αS)-1-((R)-1-((S)-3-hydroxy-2,3-dimethylbutoxy)ethyl)-7α-methyldihydro-1H-inden-4(2H,5H,6H,7H,7αH)-ylidene)ethylidene)-2-methylenecyclohexane-1,3-diol). Preparation of a-ring phenylphosphine oxide 11, followed by Wittig-Horner coupl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen B,Kawai M,Wu-Wong JR

更新日期：2013-11-01 00:00:00

abstract：:A novel series of imidazo[1,5-a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused primarily on dialkylamino side chain optimization. SAR of the aryl and small alkyl substituents was also explored. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hartz RA,Gilligan PJ,Nanda KK,Tebben AJ,Fitzgerald LW,Miller K

更新日期：2002-02-11 00:00:00