Recent advances in natural antifungal flavonoids and their derivatives.

abstract：:Derivatives of phaeosphaeride A (PPA) were synthesised and characterised; then anti-cancer studies were carried out on the A549 cancer cell line. It was found that the acetyl derivative (compound 3) displayed comparable in vitro cytotoxicity to that of PPA (EC50=49±7 μM and EC50=46±5 μM, respectively), while chloroace...

journal_title：Bioorganic & medicinal chemistry letters

authors： Abzianidze VV,Prokofieva DS,Chisty LA,Bolshakova KP,Berestetskiy AO,Panikorovskii TL,Bogachenkov AS,Holder AA

更新日期：2015-12-01 00:00:00

abstract：:A novel series of N-arylidene-2-(2,4-dichloro phenyl)-1-propyl-1H-benzo[d] imidazole-5-carbohydrazides having different substitution on the arylidene part were synthesized in good yield. The core nucleus benzimidazole-5-carboxylate (5) was efficiently synthesized by 'one-pot' nitro reductive cyclization reaction betwe...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vasantha K,Basavarajaswamy G,Vaishali Rai M,Boja P,Pai VR,Shruthi N,Bhat M

更新日期：2015-04-01 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：:Backbone-modified DNA analogs were synthesized in good yields by the boranophosphotriester method on a solid support. The oligodeoxyribonucleoside boranophosphates, protected with 2-(azidomethyl)benzoyl groups for nucleobases, were converted into DNA and its backbone-modified analogs via the corresponding H-phosphonat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kawanaka T,Shimizu M,Shintani N,Wada T

更新日期：2008-07-01 00:00:00

abstract：:SAR exploration at C-6 and C-8 positions of the tricyclic sulfone series was carried out. Several functional groups were found to be well tolerated at C-6 and C-8 positions. Selective combination of C-6 and C-8 modification resulted in new tricyclic sulfone analogs with efficacy in in vivo mouse Aβ(40) lowering model....

journal_title：Bioorganic & medicinal chemistry letters

authors： Su J,Tang H,McKittrick BA,Xu R,Clader JW,Greenlee WJ,Hyde L,Zhang L

更新日期：2011-06-01 00:00:00

abstract：:Introduction of a nitrogen atom into the 6-position of a series of pyrazolo[3,4-b]pyridines led to a dramatic improvement in the potency of GSK-3 inhibition. Rationalisation of the binding mode suggested participation of a putative structural water molecule, which was subsequently confirmed by X-ray crystallography. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Witherington J,Bordas V,Haigh D,Hickey DM,Ife RJ,Rawlings AD,Slingsby BP,Smith DG,Ward RW

更新日期：2003-05-05 00:00:00

abstract：:A series of molecules with dual inhibitory activities on calpain and lipid peroxidation were synthesized. These hybrid compounds were built on the calpain pharmacophore 2-hydroxytetrahydrofuran linked to a set of antioxidants via a l-leucine linker. Compound 7, the most potent in cellular calpain and lipid peroxidatio...

journal_title：Bioorganic & medicinal chemistry letters

authors： Auvin S,Pignol B,Navet E,Pons D,Marin JG,Bigg D,Chabrier PE

更新日期：2004-07-16 00:00:00

abstract：:The synthesis and pharmacological activity of novel nociceptin/orphanin FQ (N/OFQ) analogues modified in the Phe(1)-Gly(2) peptide bond are reported. The aim of the present work was to elucidate the importance of this peptide bond for the N/OFQ receptor (NOP) interaction. Our study indicates that the first peptide bon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guerrini R,Rizzi D,Zucchini M,Tomatis R,Regoli D,Calo' G,Salvadori S

更新日期：2003-02-10 00:00:00

abstract：:A facile 1,3-dipolar cycloaddition of azomethine ylide generated in situ from the reaction of 1,3-thiazolane-4-carboxylic acid and isatin to 2-arylidene-1,3-indanediones furnished novel dispiro-oxindolylpyrrolothiazoles regio- and stereo-selectively in moderate to good yields (60-92%). In vitro antitubercular screenin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Maheswari SU,Balamurugan K,Perumal S,Yogeeswari P,Sriram D

更新日期：2010-12-15 00:00:00

abstract：:A series of mechanism-based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Keith JM,Jones W,Pierce JM,Seierstad M,Palmer JA,Webb M,Karbarz M,Scott BP,Wilson SJ,Luo L,Wennerholm M,Chang L,Rizzolio M,Rynberg R,Chaplan S,Guy Breitenbucher J

更新日期：2020-10-15 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：:Caffeic acid derivatives are increasingly regarded as potential oncoprotective that could inhibit both the initiation and progression of cancer. Here we have synthesized seven 1-arylnaphthalene lignans and related compounds and tested their impact on breast cancer cell growth in tissue culture. The product of the oxid...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bailly F,Toillon RA,Tomavo O,Jouy N,Hondermarck H,Cotelle P

更新日期：2013-01-15 00:00:00

abstract：:A novel neurokinin-1 receptor antagonist, (+/-)-(1R( *),3S( *),4S( *),5S( *))-4-[(N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-3-phenyl-2-aza-7-oxabicyclo[3.3.0]octane (1), was synthesized stereoselectively using Padwa's intramolecular 1,3-dipolar cycloaddition methodology as the key step. Compound (+/-)-1 showed high...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shishido Y,Ito F,Morita H,Ikunaka M

更新日期：2007-12-15 00:00:00

abstract：:A series of oxazole-substituted indanylacetic acids were prepared which show a spectrum of activity as ligands for PPAR nuclear receptor subtypes. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lowe DB,Bifulco N,Bullock WH,Claus T,Coish P,Dai M,Dela Cruz FE,Dickson D,Fan D,Hoover-Litty H,Li T,Ma X,Mannelly G,Monahan MK,Muegge I,O'Connor S,Rodriguez M,Shelekhin T,Stolle A,Sweet L,Wang M,Wang Y,Zhang C

更新日期：2006-01-15 00:00:00

abstract：:Cyanobacteria possess a unique capacity for the production of structurally novel secondary metabolites compared to the biosynthetic abilities of other environmental prokaryotes such as bacteria of the genus Streptomyces. Two different strategies to explore cyanobacteria-derived natural products have been explored prev...

journal_title：Bioorganic & medicinal chemistry letters

authors： Harms H,Kurita KL,Pan L,Wahome PG,He H,Kinghorn AD,Carter GT,Linington RG

更新日期：2016-10-15 00:00:00

abstract：:This Letter details our efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxamide cores, we investigated a plethora of core replacements. This exe...

journal_title：Bioorganic & medicinal chemistry letters

authors： Temple KJ,Engers JL,Long MF,Watson KJ,Chang S,Luscombe VB,Jenkins MT,Rodriguez AL,Niswender CM,Bridges TM,Conn PJ,Engers DW,Lindsley CW

更新日期：2020-02-01 00:00:00

abstract：:We previously reported on the monobody E1, which specifically targets the tumor marker hEphA2. In this study, we labeled NOTA-conjugated E1 with 64Cu (64Cu-NOTA-E1) and evaluated biologic characteristics. The uptake of 64Cu-NOTA-E1 in PC3 cells (a human prostate cancer cell line) with high expression of hEphA2 increas...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pyo A,You SH,Sik Kim H,Young Kim J,Min JJ,Kim DY,Hong Y

更新日期：2020-07-15 00:00:00

abstract：:The discovery of PPAR antagonists is emerging as an useful tool for elucidating the biological role of the receptor. Here we report the identification of N-(phenylsulfonyl)amides containing the benzothiazole scaffold, a novel class of potent PPARα antagonists obtained from chemical modification of carboxylic acid agon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ammazzalorso A,Giancristofaro A,D'Angelo A,Filippis BD,Fantacuzzi M,Giampietro L,Maccallini C,Amoroso R

更新日期：2011-08-15 00:00:00

abstract：:We report the results of our study into a series of simple phenyl and alkyl sulfamates and alkyl methanesulfonates as potential inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that the substituted phenyl sulfamates are good irreversible inhibitors; the alkyl sulfamate compounds were foun...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ahmed S,James K,Owen CP,Patel CK,Sampson L

更新日期：2002-05-06 00:00:00

abstract：:This communication describes the high-throughput screen of a diverse library of 50,000 small molecules against Escherichia coli dihydrofolate reductase to detect inhibitors. Sixty-two compounds were identified as having significant inhibitory activity against the enzyme. Secondary screening of these revealed twelve mo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zolli-Juran M,Cechetto JD,Hartlen R,Daigle DM,Brown ED

更新日期：2003-08-04 00:00:00

abstract：:Tripeptide-derived molecules incorporating C-terminal ketone electrophiles were evaluated as reversible inhibitors of the cysteine-containing human rhinovirus 3C protease (3CP). An optimized example of such compounds displayed potent 3CP inhibition activity (K = 0.0045 microM) and in vitro antiviral properties (EC50=0...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dragovich PS,Zhou R,Webber SE,Prins TJ,Kwok AK,Okano K,Fuhrman SA,Zalman LS,Maldonado FC,Brown EL,Meador JW 3rd,Patick AK,Ford CE,Brothers MA,Binford SL,Matthews DA,Ferre RA,Worland ST

更新日期：2000-01-03 00:00:00

abstract：:The chiral analogues of gemfibrozil 5-(2,5-dimethylphenoxy)-2-methylpentanoic acid and 5-(2,5-dimethylphenoxy)-2-ethylpentanoic acid were synthesized in optically active form using (S)-4-(1-methylethyl)-2-oxazolidinone as chiral auxiliary. All compounds inhibit human platelet aggregation. From these data, one can surm...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ammazzalorso A,Amoroso R,Baraldi M,Bettoni G,Braghiroli D,De Filippis B,Duranti A,Moretti M,Tortorella P,Tricca ML,Vezzalini F

更新日期：2002-03-11 00:00:00

abstract：:The Keap1-Nrf2 system is involved not only in biological defense but also in malignancy progression and chemoresistance. The ubiquitin-binding protein p62/Sqstm1 (p62), which is highly expressed in several cancers, competes with Nrf2 for Keap1 binding, leading to activation of Nrf2-mediated gene expression and surviva...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yasuda D,Nakajima M,Yuasa A,Obata R,Takahashi K,Ohe T,Ichimura Y,Komatsu M,Yamamoto M,Imamura R,Kojima H,Okabe T,Nagano T,Mashino T

更新日期：2016-12-15 00:00:00

abstract：:Several 1-[(2-hydroxy-ethoxy)methyl]-3-carbethoxy-4(1H)quinolones (2a-l) and l-[(2-hydroxy-ethoxy)methyl]-4(1H)quinolone-3-carboxylic acids (3a-j and 3l) were synthesized and 2a-j, 2l and 3a-j, 3l were evaluated against herpes simplex virus type 1 (HSV-1), employing a one-pot reaction: silylation of the desired quinol...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lucero Bd,Gomes CR,Frugulhetti IC,Faro LV,Alvarenga L,de Souza MC,de Souza TM,Ferreira VF

更新日期：2006-02-15 00:00:00

abstract：:Aiming to develop a new (99m)Tc-labeled folate derivative for FR-positive tumor imaging, a simpler method has been established to synthesize the folate-drug conjugates with free α-carboxyl group. In this study, the conjugate pteroyl-lys-HYNIC was synthesized and labeled with (99m)Tc using tricine and TPPTS as co-ligan...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guo H,Xie F,Zhu M,Li Y,Yang Z,Wang X,Lu J

更新日期：2011-04-01 00:00:00

abstract：:The first total synthesis of 6(E),8(Z),11(Z),13(E) 5-oxo-15-HETE 4 was accomplished. The synthetic material was evaluated with calcium mobilization assay and compared with 5-oxo-ETE the natural ligand for the OXE receptor. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patel P,Anumolu JR,Powell WS,Rokach J

更新日期：2011-03-15 00:00:00

abstract：:The synthesis and biological evaluation of a series of novel isobenzofuran-based compounds are described. The compounds were evaluated for their immunosuppressive effects of T-cell proliferation and IMPDH type II inhibitor activity in vitro, as well as their structure-activity relationships were assessed. Several comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang N,Wang QH,Wang WQ,Wang J,Li F,Tan SP,Cheng MS

更新日期：2012-01-01 00:00:00

abstract：:Resistance of malaria parasites has quickly developed to almost all used antimalarial drugs. Accordingly, the discovery of new effective drugs to counter the spread of malaria parasites that are resistant to existing agents, especially acting on multi-targets, is an urgent need. The cysteine protease falcipain-2 (FP-2...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang H,Lu W,Li X,Cong X,Ma H,Liu X,Zhang Y,Che P,Ma R,Li H,Shen X,Jiang H,Huang J,Zhu J

更新日期：2012-01-15 00:00:00

abstract：:A series of sixteen β-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-β-carboline and various aldehydes under basic conditions followed by N2-alkylation using different alkyl bromides. The prepared compounds were evaluated for in vitro cytotoxicity against a panel of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venkataramana Reddy PO,Hridhay M,Nikhil K,Khan S,Jha PN,Shah K,Kumar D

更新日期：2018-05-01 00:00:00

abstract：:Two new oligostilbenes, caragasinins A (5) and B (10), and eight known compounds, kobophenol A (1), (+)-α-viniferin (2), (+)-ampelopsin F (3), pallidol (4), (+)-isoampelopsin F (6), miyabenol C (7), carasinaurone (8) and caraphenol B (9) were isolated from the ethylacetate-soluble extract of the roots of Caragana sini...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin Q,Han XH,Hong SS,Lee C,Choe S,Lee D,Kim Y,Hong JT,Lee MK,Hwang BY

更新日期：2012-01-15 00:00:00