Synthesis and structure evaluation of a novel cantharimide and its cytotoxicity on SK-Hep-1 hepatoma cells.


:A remarkable control of the potency of cantharimide is described based on the electronic properties of functional group and it exhibits a relatively less toxic effect to the non-malignant hematological disorder bone marrow cells.


Bioorg Med Chem Lett


Kok SH,Chui CH,Lam WS,Chen J,Lau FY,Wong RS,Cheng GY,Lai PB,Leung TW,Yu MW,Tang JC,Chan AS




Has Abstract


2007-03-01 00:00:00














  • Fluorescent diphenylphosphonate-based probes for detection of serine protease activity during inflammation.

    abstract::Activity-based probes are small molecules that covalently bind to the active site of a protease in an activity-dependent manner. We synthesized and characterized two fluorescent activity-based probes that target serine proteases with trypsin-like or elastase-like activity. We assessed the selectivity and potency of th...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Edgington-Mitchell LE,Barlow N,Aurelio L,Samha A,Szabo M,Graham B,Bunnett N

    更新日期:2017-01-15 00:00:00

  • Facile synthesis and 18F-radiolabeling of α4β1-specific LLP2A-aryltrifluoroborate peptidomimetic conjugates.

    abstract::The peptidomimetic, LLP2A, is a specific, high-affinity ligand for α4β1 integrin receptors. Previously, several PEGylated LLP2A conjugates were evaluated in vivo as imaging agents for the detection of lymphoma, leukemia, multiple myeloma and melanoma tumours via NIR-fluorescence, 111In-SPECT, and 64Cu- and 68Ga-PET im...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Walker D,Li Y,Roxin Á,Schaffer P,Adam MJ,Perrin DM

    更新日期:2016-10-15 00:00:00

  • Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90.

    abstract::Described are the syntheses of three sansalvamide A derivatives that contain biotinylated tags at individual positions around the macrocycle. The tagged derivatives indicated in protein pull-down assays that they bind to Hsp90 at the same binding site (N-Middle domain) as the San A-amide peptide. Further, these compou...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Kunicki JB,Petersen MN,Alexander LD,Ardi VC,McConnell JR,McAlpine SR

    更新日期:2011-08-15 00:00:00

  • Synthesis of pyrazole peptidomimetics and their inhibition against A549 lung cancer cells.

    abstract::A series of novel pyrazole peptidomimetics was synthesized from 3-aryl-1-arylmethyl-1H-pyrazole-5-carboxylic acid and amino acid ester. Structures of the compounds were characterized by means of IR, (1)H NMR and mass spectroscopy. Compounds 5e and 5k suppress effectively the growth of A549 lung cancer cells. Prelimina...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Liu YR,Luo JZ,Duan PP,Shao J,Zhao BX,Miao JY

    更新日期:2012-11-15 00:00:00

  • Structure-activity relationship of potent antimicrobial peptide analogs of Ixosin-B amide.

    abstract::There is a great urgency in developing a new generation of antibiotics and antimicrobial agents since the bacterial resistance to antibiotics have increased dramatically. A series of overlapped peptide fragments of Ixosin-B, an antimicrobial peptide with amino acid sequence of QLKVDLWGTRSGIQPEQHSSGKSDVRRWRSRY, was des...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Wu YS,Liao ZJ,Wang KS,Lung FD

    更新日期:2013-05-15 00:00:00

  • Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.

    abstract::The rational design, syntheses and evaluation of potent sulfonamidopyrrolidin-2-one-based factor Xa inhibitors incorporating aminoindane and phenylpyrrolidine P4 motifs are described. These series delivered highly potent anticoagulant compounds with excellent oral pharmacokinetic profiles; however, significant time de...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Young RJ,Adams C,Blows M,Brown D,Burns-Kurtis CL,Chan C,Chaudry L,Convery MA,Davies DE,Exall AM,Foster G,Harling JD,Hortense E,Irvine S,Irving WR,Jackson S,Kleanthous S,Pateman AJ,Patikis AN,Roethka TJ,Senger S,

    更新日期:2011-03-15 00:00:00

  • Antiproliferative activity of 2,3-disubstituted indoles toward apoptosis-resistant cancers cells.

    abstract::Many types of cancer, including glioma, melanoma, NSCLC, among others, are resistant to apoptosis induction and poorly responsive to current therapies with propaptotic agents. We describe a series of 2,3-disubstituted indoles, which display cytostatic rather than cytotoxic effects in cancer cells, and serve as a new c...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Magedov IV,Lefranc F,Frolova LV,Banuls LM,Peretti AS,Rogelj S,Mathieu V,Kiss R,Kornienko A

    更新日期:2013-06-01 00:00:00

  • Synthesis and anti-tumor activity study of water-soluble PEG-celastrol coupling derivatives as self-assembled nanoparticles.

    abstract::To improve the drug-ability of celastrol, a series of PEGylation celastrol (PEGC) were designed and synthesized by conjugation with different kinds of polyethylene glycols (PEGs) with celastrol. Most of PEGCs could easily dissolve in water. In particular, one of them (DC1000) could be dispersed in water to form nanopa...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Shan WG,Wang HG,Wu R,Zhan ZJ,Ma LF

    更新日期:2019-03-01 00:00:00

  • Evaluation of steroidal amines as lipid raft modulators and potential anti-influenza agents.

    abstract::The influenza A virus (IFV) possesses a highly ordered cholesterol-rich lipid envelope. A specific composition and structure of this membrane raft envelope are essential for viral entry into cells and virus budding. Several steroidal amines were investigated for antiviral activity against IFV. Both, a positively charg...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Agarwal S,Schroeder C,Schlechtingen G,Braxmeier T,Jennings G,Knölker HJ

    更新日期:2013-09-15 00:00:00

  • The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold.

    abstract::Glucokinase is a key enzyme in glucose homeostasis since it phosphorylates glucose to give glucose-6-phosphate, which is the first step in glycolysis. GK activators have been proven to lower blood-glucose, and therefore have potential as treatments for type 2 diabetes. Here the discovery of pyrazolopyrimidine GKAs is ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Bonn P,Brink DM,Fägerhag J,Jurva U,Robb GR,Schnecke V,Svensson Henriksson A,Waring MJ,Westerlund C

    更新日期:2012-12-15 00:00:00

  • Small-molecule microarrays: development of novel linkers and an efficient detection method for bound proteins.

    abstract::Novel isocyanate and diazoketone linkers possessing polyoxypropylenediamine as a spacer for small-molecule microrray are developed. White light interferometry is introduced to detect bound proteins on the glass slides without using chemically modified proteins. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Kurosu M,Mowers WA

    更新日期:2006-07-01 00:00:00

  • Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs.

    abstract::5-(2,8-Bis(trifluoromethyl)quinolin-4-yloxymethyl)isoxazole-3-carboxylic acid ethyl ester (compound 3) was reported to have excellent antituberculosis activity against both replicating and non-replicating Mycobacterium tuberculosis, with a minimum inhibitory concentration (MIC) of 0.9 microM and 12.2 microM, respectiv...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Mao J,Yuan H,Wang Y,Wan B,Pak D,He R,Franzblau SG

    更新日期:2010-02-01 00:00:00

  • Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.

    abstract::Amidino-phenoxy quinoline derivatives represent a new class of potent thrombin inhibitors with good selectivity and remarkably low molecular weight (M(W): 335-391). X-ray analyses of thrombin-bound inhibitors revealed that enzyme inhibition is mainly based on hydrophobic interactions. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Ries UJ,Priepke HW,Hauel NH,Haaksma EE,Stassen JM,Wienen W,Nar H

    更新日期:2003-07-21 00:00:00

  • Rhodanine-3-acetic acid derivatives as inhibitors of fungal protein mannosyl transferase 1 (PMT1).

    abstract::The first inhibitors of fungal protein: mannosyl transferase 1 (PMT1) are described. They are based upon rhodanine-3-acetic acid and several compounds have been identified, for example, 5-[[3-(1-phenylethoxy)-4-(2-phenylethoxy)phenyl]methylene]-4-oxo-2-thioxo-3-thiazolidineacetic acid (5a), which inhibit Candida albic...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Orchard MG,Neuss JC,Galley CM,Carr A,Porter DW,Smith P,Scopes DI,Haydon D,Vousden K,Stubberfield CR,Young K,Page M

    更新日期:2004-08-02 00:00:00

  • Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.

    abstract::Structure-activity relationship studies for two series of 2-benzyloxy-5-(4-chlorophenyl)-6-(2,4-dichlorophenyl)pyridines having either a 3-cyano or 3-carboxamide moiety resulted in the preparation of the 2-(3,4-difluorobenzyloxy)-3-nitrile analog 10d and the 2-(3,4-difluorobenzyloxy)-3-(N-propylcarboxamide) analog 16c...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Meurer LC,Finke PE,Mills SG,Walsh TF,Toupence RB,Debenham JS,Goulet MT,Wang J,Tong X,Fong TM,Lao J,Schaeffer MT,Chen J,Shen CP,Sloan Stribling D,Shearman LP,Strack AM,Van der Ploeg LH

    更新日期:2005-02-01 00:00:00

  • Synthesis and characterisation of a new amphotericin B-methoxypoly(ethylene glycol) conjugate.

    abstract::The reaction of methoxypoly(ethylene glycol)-4-nitrophenyl carbonate with amphotericin B has been used to prepare a new conjugate of amphotericin B (mPEG-AmB). A preliminary screening of in vitro antifungal activity has suggested that mPEG-AmB possesses a similar effect and a similar spectrum of activity as the conven...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Sedlák M,Buchta V,Kubicová L,Simůnek P,Holcapek M,Kasparová P

    更新日期:2001-11-05 00:00:00

  • Hydroxyl radicals scavenging activity of N-substituted chitosan and quaternized chitosan.

    abstract::N-substituted chitosan and quaternized chitosan were synthesized and their antioxidant activity against hydroxyl radicals was assessed, respectively. Compared with the antioxidant activity of chitosan, the results indicated that the two kinds of chitosan derivatives had different scavenging ability on hydroxyl radical...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Guo Z,Liu H,Chen X,Ji X,Li P

    更新日期:2006-12-15 00:00:00

  • Inhaled Janus Kinase (JAK) inhibitors for the treatment of asthma.

    abstract::Multiple asthma-relevant cytokines including IL-4, IL-5, IL-13, and TSLP depend upon JAKs for signaling. JAK inhibition may, therefore, offer a novel intervention strategy for patients with disease refractory to current standards of care. Multiple systemically delivered JAK inhibitors have been approved for human use ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章,评审


    authors: Zak M,Dengler HS,Rajapaksa NS

    更新日期:2019-10-15 00:00:00

  • Synthesis and quantitative structure-activity relationship (QSAR) analysis of some novel oxadiazolo[3,4-d]pyrimidine nucleosides derivatives as antiviral agents.

    abstract::We have synthesized a series of 4H,6H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleoside and their anti-vesicular stomatitis virus (VSV) activities in Wish cell were also investigated in vitro. It was found that most compounds showed obvious anti-VSV activities and compound 9 with ribofuranoside improved ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Xu X,Wang J,Yao Q

    更新日期:2015-01-15 00:00:00

  • Antimalarial activity of tetrahydro-β-carbolines targeting the ATP binding pocket of the Plasmodium falciparum heat shock 90 protein.

    abstract::A series of tetrahydro-β-carboline derivatives of a lead compound known to target the heat shock 90 protein of Plasmodium falciparum were synthesized and assayed for both potency against the parasite and toxicity against a human cell line. Using a rationalized structure based design strategy, a new lead compound with ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Eagon S,Hammill JT,Bach J,Everson N,Sisley TA,Walls MJ,Durham S,Pillai DR,Falade MO,Rice AL,Kimball JJ,Lazaro H,DiBernardo C,Kiplin Guy R

    更新日期:2020-11-01 00:00:00

  • Glycan multivalency effects toward albumin enable N-glycan-dependent tumor targeting.

    abstract::Multivalent interactions play an essential role in molecular recognition in living systems. These effects were employed to target tumor cells using albumin clusters bearing ∼10 molecules of asparagine-linked glycans (N-glycans). Noninvasive near-infrared fluorescence imaging clearly revealed A431 tumors implanted in B...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Ogura A,Tahara T,Nozaki S,Onoe H,Kurbangalieva A,Watanabe Y,Tanaka K

    更新日期:2016-05-01 00:00:00

  • Synthesis of cholestane glycosides bearing OSW-1 disaccharide or its 1-->4-linked analogue and their antitumor activities.

    abstract::For further structure-activity relationship (SAR) research of OSW saponins, a cholestane glycoside, namely 3beta, 16beta, 26-trihydroxycholest-5-en-22-one 16-O-(2-O-4-methoxybenzoyl-beta-D-xylopyranosyl)-(1-->3)-2-O-acetyl-alpha-L-arabinopyranoside (1) together with two 1-->4-linked disaccharide analogues (2 and 3) we...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Zheng D,Zhou L,Guan Y,Chen X,Zhou W,Chen X,Lei P

    更新日期:2010-09-15 00:00:00

  • Chiral synthesis and pharmacological evaluation of NPS 1407: a potent, stereoselective NMDA receptor antagonist.

    abstract::The stereoselective synthesis and biological activity of NPS 1407 (4a), (S)-(-)-3-amino-1,1-bis(3-fluorophenyl)butane, a potent, stereoselective antagonist of the NMDA receptor, are described. The racemate (4) was found to be active at the NMDA receptor in an in vitro assay, prompting the synthesis of the individual s...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Moe ST,Smith DL,DelMar EG,Shimizu SM,Van Wagenen BC,Balandrin MF,Chien YE,Raszkiewicz JL,Artman LD,White HS,Mueller AL

    更新日期:2000-11-06 00:00:00

  • Theoretical elucidation on structure-antioxidant activity relationships for indolinonic hydroxylamines.

    abstract::Indolinonic hydroxylamines (IH), representing a new type of antioxidants, are comparative to alpha-tocopherol to protect lipids from oxidation. To elucidate the structure-activity relationship for IH, B3LYP/6-31G(d, p) method was employed to calculate the O-H bond dissociation enthalpy (BDE), a theoretical parameter t...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Zhang HY,Wang LF

    更新日期:2002-01-21 00:00:00

  • Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.

    abstract::Structural features of the substituted 4-piperidinyl urea analogs 1, responsible for the H3 antagonist activity, have been identified. Structure-activity relationship of the H3 receptor affinity, hERG ion channel inhibitory activity and their separation is described. Preliminary pharmacokinetic evaluation of the compo...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Berlin M,Lee YJ,Boyce CW,Wang Y,Aslanian R,McCormick KD,Sorota S,Williams SM,West RE Jr,Korfmacher W

    更新日期:2010-04-01 00:00:00

  • Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: tuning of receptor selectivity and in vivo efficacy.

    abstract::In the previous article we demonstrated how certain CCK2R-selective anthranilic amides could be structurally modified to afford high-affinity, selective CCK1R activity. We now describe our efforts at modulating and optimizing the CCK1R and CCK2R affinities aimed at producing compounds with good pharmacokinetics proper...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Pippel M,Boyce K,Venkatesan H,Phuong VK,Yan W,Barrett TD,Lagaud G,Li L,Morton MF,Prendergast C,Wu X,Shankley NP,Rabinowitz MH

    更新日期:2009-11-15 00:00:00

  • Phenolic P2/P3 core motif as thrombin inhibitors--design, synthesis, and X-ray co-crystal structure.

    abstract::Prototypical thrombin inhibitors were synthesized based on a trisubstituted phenol as a core motif. A naphthylsulfonamide analogue showed excellent antithrombin activity. An X-ray co-crystal structure showed the expected interactions. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Hanessian S,Therrien E,van Otterlo WA,Bayrakdarian M,Nilsson I,Fjellström O,Xue Y

    更新日期:2006-02-15 00:00:00

  • Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases.

    abstract::Pyrimido-oxazepine based sub-micromolar inhibitors (2-4) for Aurora and FLT-3 were designed and synthesized. These preliminary results supported the potential use of pyrimido-oxazepines as a versatile template for developing specific kinase inhibitors. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Pan W,Liu H,Xu YJ,Chen X,Kim KH,Milligan DL,Columbus J,Hadari YR,Kussie P,Wong WC,Labelle M

    更新日期:2005-12-15 00:00:00

  • Respiratory syncytial virus fusion inhibitors. Part 5: Optimization of benzimidazole substitution patterns towards derivatives with improved activity.

    abstract::Extensive SAR studies and optimization of ADME properties of benzimidazol-2-one derivatives led to the identification of BMS-433771 (3) as an orally active RSV fusion inhibitor. In order to extend the structure-activity relationships for this compound series, substitution of the benzimidazole ring was examined with a ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Wang XA,Cianci CW,Yu KL,Combrink KD,Thuring JW,Zhang Y,Civiello RL,Kadow KF,Roach J,Li Z,Langley DR,Krystal M,Meanwell NA

    更新日期:2007-08-15 00:00:00

  • 5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.

    abstract::A series of 5-aminomethylquinoxaline-2,3-diones have been identified as potent and selective AMPA antagonists. Some of these compounds are also active at the glycine-binding site of the NMDA receptors. A number of these novel, water-soluble quinoxaline-2,3-dione derivatives display protective effects in the electrosho...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Auberson YP,Bischoff S,Moretti R,Schmutz M,Veenstra SJ

    更新日期:1998-01-06 00:00:00