Macrocarpins A-D, new cytotoxic nor-triterpenes from Maytenus macrocarpa.

abstract：:Imidazoline-based small molecule inhibitors of p53-MDM2 interaction intended for the treatment of p53 wild-type tumors are the promising structures for design of anticancer drugs. Based on fragment approach we have investigated a key role of substituents in cis-imidazoline core for biological activity of nutlin family...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bazanov DR,Pervushin NV,Savitskaya VY,Anikina LV,Proskurnina MV,Lozinskaya NA,Kopeina GS

更新日期：2019-08-15 00:00:00

abstract：:A new series of polyhydroxylated N-benzylbenzamide derivatives containing an adamantyl moiety has been synthesized, and the depigmenting and tyrosinase inhibitory activities of the molecules were evaluated. The lipophilic character of the adamantyl moiety appeared to confer greater depigmentation power on the benzamid...

journal_title：Bioorganic & medicinal chemistry letters

authors： Baek HS,Hong YD,Lee CS,Rho HS,Shin SS,Park YH,Joo YH

更新日期：2012-03-01 00:00:00

abstract：:The synthesis of a 20 member 2-aminoimidazole/triazole pilot library is reported. Each member of the library was screened for its ability to inhibit or promote biofilm development of either Escherichia coli and Acinetobacter baumannii. From this screen, E. coli-selective 2-aminoimidazoles were discovered, with the bes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Reed CS,Huigens RW 3rd,Rogers SA,Melander C

更新日期：2010-11-01 00:00:00

abstract：:We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Quan ML,Pinto DJ,Rossi KA,Sheriff S,Alexander RS,Amparo E,Kish K,Knabb RM,Luettgen JM,Morin P,Smallwood A,Woerner FJ,Wexler RR

更新日期：2010-02-15 00:00:00

abstract：:Cu (II) complex with 1,4,7,10-tetrakis(2-cyanoethyl-)-1,4,7,10-tetraazacyclododecane was prepared and characterized by X-ray diffraction. Four nitrogen atoms of macrocyclic ligand and oxygen atom of water molecule defined a tetragonal pyramidal polyhedron surrounding the central copper atom. Preliminary pharmacologica...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kong D,Qin C,Meng L,Xie Y

更新日期：1999-04-19 00:00:00

abstract：:Ureas derived from two substituted 3-aminopyrrolidine subunits were prepared as constrained analogs of a linear lead compound and tested as antagonists of the MCH(1) receptor. The series was optimized for substitution and stereochemistry to generate a functional antagonist with a K(i) of 3.3 nM and IC(50) of 12 nM (GT...

journal_title：Bioorganic & medicinal chemistry letters

authors： Grey J,Dyck B,Rowbottom MW,Tamiya J,Vickers TD,Zhang M,Zhao L,Heise CE,Schwarz D,Saunders J,Goodfellow VS

更新日期：2005-02-15 00:00:00

abstract：:Novel 6,8-difluoro-1-alkyl-5-amino-1,4-dihydro-4-oxo-7-{4-substituted piperazin-1-yl}-quinoline-3-carboxylic acids, with the substituents at 4th position of piperazine being -[2(pyridine-4-carbonyl) hydrazono]propyl and -2 [(pyrazine-2-carbonyl) amino] ethyl, were synthesized and evaluated in vivo against Mycobacteriu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shindikar AV,Viswanathan CL

更新日期：2005-04-01 00:00:00

abstract：:The diastereoselective synthesis and structure activity relationship (SAR) of a series of fused cyclopropyl-3-amino-2,4-oxazine (2-oxa-4-azabicyclo[4.1.0]hept-3-en-3-amine)-containing BACE inhibitors is described. Through these efforts compound 2 was identified as a potent (cell IC50 = 15 nM) BACE inhibitor with accep...

journal_title：Bioorganic & medicinal chemistry letters

authors： Low JD,Bartberger MD,Cheng Y,Whittington D,Xue Q,Wood S,Allen JR,Minatti AE

更新日期：2018-04-01 00:00:00

abstract：:A newly designed curcumin mimic library (11a-11k) with 2-ethylamino groups in a chalcone structure and variously substituted triazole groups as side chains was synthesized using the Huisgen 1,3-cycloaddition reaction between various alkynes (a-k) and an intermediate (10), with CuSO4 and sodium ascorbate in a solution ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ahn Y,Oh S,Lee SJ,Park BG,Park YS,Shin WS,Jang HJ,Park JH,Kwon D,Lee S

更新日期：2014-08-01 00:00:00

abstract：:Reaction of 7-amino-9-ethylguaninium chloride with lead(IV) acetate (LTA) in MeOH yielded 8-aza-9-ethylguanine. Similarly, the reaction of 1-amino-3-methylbenzimidazolium chloride or its substituted derivatives (6-methyl, 5,6-dimethyl and 5-nitro) with LTA gave the corresponding 1-methyl-1H-benzotriazole (or 1-methyl-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kaiya T,Aoyama S,Kohda K

更新日期：1999-04-05 00:00:00

abstract：:This Letter describes the chemical optimization of a novel series of M4 positive allosteric modulators (PAMs) based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core, identified from an MLPCN functional high-throughput screen. The HTS hit was potent and selective, but not CNS penetrant. Potency was main...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wood MR,Noetzel MJ,Engers JL,Bollinger KA,Melancon BJ,Tarr JC,Han C,West M,Gregro AR,Lamsal A,Chang S,Ajmera S,Smith E,Chase P,Hodder PS,Bubser M,Jones CK,Hopkins CR,Emmitte KA,Niswender CM,Wood MW,Duggan ME,C

更新日期：2016-07-01 00:00:00

abstract：:Histone deacetylase (HDAC) inhibitors modulate various cellular functions including proliferation, differentiation, and apoptosis. Vorinostat (SuberAniloHydroxamic Acid, SAHA) is the first HDAC inhibitor approved by FDA for cancer treatment. However, SAHA distributes in cancer tissue and normal tissue in similar level...

journal_title：Bioorganic & medicinal chemistry letters

authors： Idippily ND,Gan C,Orefice P,Peterson J,Su B

更新日期：2017-02-15 00:00:00

abstract：:Human isoprenylcysteine carboxyl methyltransferase (hIcmt) is a promising anticancer target as it is important for the post-translational modification of oncogenic Ras proteins. We herein report the synthesis and biochemical activity of 41 farnesyl-cysteine based analogs versus hIcmt. We have demonstrated that the ami...

journal_title：Bioorganic & medicinal chemistry letters

authors： Majmudar JD,Hahne K,Hrycyna CA,Gibbs RA

更新日期：2011-05-01 00:00:00

abstract：:A series of 1,4-benzyloxybenzylsulfanylaryl carboxylic acids were prepared and their activities for PPAR receptor subtypes (alpha, delta, and gamma) with potential indications for the treatment of dyslipidemia were investigated. Analog 13a displayed the greatest binding affinity (IC(50)=10nM) and selectivity (120-fold...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bratton LD,Filzen GF,Geyer A,Hoffman JK,Lu G,Pulaski J,Trivedi BK,Unangst PC,Xu X

更新日期：2007-07-01 00:00:00

abstract：:The design and synthesis of new 1alpha,25-dihydroxy-19-norvitamin D(3) analogues 3a-c, which have an amide bond in the molecule instead of the diene, are described. The A-ring moiety was constructed by a (3S,5S)-3,5-dihydroxypiperidine derivative (9, 11, or 13) prepared from D-mannose, and a CD-ring carboxylic acid 16...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suhara Y,Kittaka A,Ono K,Kurihara M,Fujishima T,Yoshida A,Takayama H

更新日期：2002-12-16 00:00:00

abstract：:The protein tyrosine kinases (PTKs) are essential enzymes in cellular signaling processes that regulate cell growth, differentiation, migration and metabolism. Their inhibition was recently shown to constitute a new modality for treating cancers. Two clinically used PTK inhibitors (PTKIs), imatinib (Glivec/Gleevec) an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parkkila S,Innocenti A,Kallio H,Hilvo M,Scozzafava A,Supuran CT

更新日期：2009-08-01 00:00:00

abstract：:Neuraminidase has been considered as an important target for designing agents against influenza viruses. In a discovery of anti-influenza agents with epigoitrin as the initial lead compound, a series of 1-amino-2-alkanols were synthesized and biologically evaluated. The in vitro evaluation indicated that (E)-1-amino-4...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lu C,Yin Y,Meng F,Dun Y,Pei K,Wang C,Xu X,Wu F

更新日期：2018-06-15 00:00:00

abstract：:Benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS) can be effectively treated by alpha(1) adrenergic receptor antagonists, but these drugs also produce side effects that are related to their subtype non-selective nature. To overcome this limitation, it was hypothesized that an alpha(1a/1d) subtype-se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chiu G,Li S,Cai H,Connolly PJ,Peng S,Stauber K,Pulito V,Liu J,Middleton SA

更新日期：2007-11-15 00:00:00

abstract：:A series of new imines and amines have been synthesized by condensation of 1H-3-ferrocenyl-1-phenylpyrazole-4-carboxaldehyde with the corresponding amines, followed by reduction with sodium borohydride. The synthesized compounds have been screened for their in vitro antimicrobial activity against 11 bacteria and three...

journal_title：Bioorganic & medicinal chemistry letters

authors： Damljanović I,Vukićević M,Radulović N,Palić R,Ellmerer E,Ratković Z,Joksović MD,Vukićević RD

更新日期：2009-02-15 00:00:00

abstract：:Novel and artificial anthraquinone-carbohydrate hybrids were designed and synthesized, and found to effectively cleave DNA under irradiation with a long wavelength UV light and also exhibit cytotoxicity against HeLa S3 cells. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Toshima K,Maeda Y,Ouchi H,Asai A,Matsumura S

更新日期：2000-10-02 00:00:00

abstract：:Herein, we reported the synthesis of 16 novel steroidal thiosemicarbazone derivatives via the condensation of steroidal ketones and substituted thiosemicarbazides under solvent-free conditions using microwave irradiation. The yields obtained are in the range of 84-96% using microwave method and 46-62% using convention...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao Z,Shi Z,Liu M,Liu X

更新日期：2012-12-15 00:00:00

abstract：:Albocycline (ALB) is a unique macrolactone natural product with potent, narrow-spectrum activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate (VISA), and vancomycin-resistant S. aureus (VRSA) strains (MIC = 0.5-1.0 μg/mL). Described herein is the synthesis and evaluation of a nov...

journal_title：Bioorganic & medicinal chemistry letters

authors： Daher SS,Franklin KP,Scherzi T,Dunman PM,Andrade RB

更新日期：2020-11-01 00:00:00

abstract：:A series of substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles has been prepared as Src kinase inhibitors. Optimal activity is observed with compounds that have basic amines attached via the para position of the 7-phenyl ring, and a hydrogen atom at the C-6 position. The best compounds are low nanomolar inhibitor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Berger D,Dutia M,Powell D,Wissner A,DeMorin F,Raifeld Y,Weber J,Boschelli F

更新日期：2002-10-21 00:00:00

abstract：:In general, serine protease chymase inhibitors readily decompose in plasma. We previously found that thiazolidine-2,4-dione and thiadiazole derivatives are also unstable. Using a pharmacophore-based database search, we identified a benzo[b]thiophen-2-sulfonamide derivative as a stable chymase inhibitor. Finding a lead...

journal_title：Bioorganic & medicinal chemistry letters

authors： Koide Y,Tatsui A,Hasegawa T,Murakami A,Satoh S,Yamada H,Kazayama S,Takahashi A

更新日期：2003-01-06 00:00:00

abstract：:5-Aminolaevulinic acid (ALA) prodrugs have been widely used in photodynamic therapy (PDT) as precursors to the natural photosensitizer, protoporphyrin IX (PpIX). The main disadvantage of this therapy is that ALA is poorly absorbed by cells due to its high hydrophilicity. In order to improve the therapeutical effect an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu CF,Battah S,Kong X,Reeder BJ,Hider RC,Zhou T

更新日期：2015-02-01 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：:Toll-like receptors (TLRs) are a type of pattern recognition receptors (PRRs), which are activated by recognizing pathogen-associated molecular patterns (PAMPs). The activation of TLRs initiates innate immune responses and subsequently leads to adaptive immune responses. TLR agonists are effective immuomodulators in v...

journal_title：Bioorganic & medicinal chemistry letters

authors： Baba A,Wakao M,Shinchi H,Chan M,Hayashi T,Yao S,Cottam HB,Carson DA,Suda Y

更新日期：2020-02-01 00:00:00

abstract：:The design and synthesis of macrocyclic inhibitors of human rhinovirus 3C protease is described. A macrocyclic linkage of the P1 and P3 residues, and the subsequent structure-based optimization of the macrocycle conformation and size led to the identification of a potent biochemical inhibitor 10 with sub-micromolar an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Namoto K,Sirockin F,Sellner H,Wiesmann C,Villard F,Moreau RJ,Valeur E,Paulding SC,Schleeger S,Schipp K,Loup J,Andrews L,Swale R,Robinson M,Farady CJ

更新日期：2018-03-01 00:00:00

abstract：:Detailed structure-activity relationships of the C3-phenyl moiety that allow for the optimization of antiviral potency of a series of 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione inhibitors of HIV capsid (CA) assembly are described. Combination of favorable substitutions gave additive SAR and allowed for the identifica...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fader LD,Landry S,Goulet S,Morin S,Kawai SH,Bousquet Y,Dion I,Hucke O,Goudreau N,Lemke CT,Rancourt J,Bonneau P,Titolo S,Amad M,Garneau M,Duan J,Mason S,Simoneau B

更新日期：2013-06-01 00:00:00

abstract：:A kinetic analysis of an enzyme assay employing a synthetic substrate that produces a detectable signal through a spontaneous organic cyclization/elimination reaction following the enzymatic reaction was conducted. The results from the calculation were used to predict the lag period and provide accurate measurements o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xue F,Seto CT

更新日期：2011-02-01 00:00:00