当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Enediynes: Exploration of microbial genomics to discover new anticancer drug leads.

Enediynes: Exploration of microbial genomics to discover new anticancer drug leads.

Abstract：

:The enediyne natural products have been explored for their phenomenal cytotoxicity. The development of enediynes into anticancer drugs has been successfully achieved through the utilization of polymer- and antibody-drug conjugates (ADCs) as drug delivery systems. An increasing inventory of enediynes would benefit current application of ADCs in many oncology programs. Innovations in expanding the enediyne inventory should take advantage of the current knowledge of enediyne biosynthesis and post-genomics technologies. Bioinformatics analysis of microbial genomes reveals that enediynes are underexplored, in particular from Actinomycetales. This digest highlights the emerging opportunities to explore microbial genomics for the discovery of novel enediyne natural products.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Shen B,Hindra,Yan X,Huang T,Ge H,Yang D,Teng Q,Rudolf JD,Lohman JR

doi

10.1016/j.bmcl.2014.11.019

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

9-15

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)01203-7

journal_volume

25

pub_type

杂志文章,评审

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Synthesis and muscarinic M(2) subtype antagonistic activity of enantiomeric pairs of 3-demethylhimbacine (3-norhimbacine) and its C(4)-epimer.

    abstract：:In the course of our studies of the structure-activity relationships of himbacine 1, a potent antagonist of the M(2) subtype of muscarinic receptor, the four title compounds, 2, ent-2, 3, and ent-3, were synthesized with a highly stereoselective intermolecular Diels-Alder reaction of tetrahydroisobenzofuran 4 with ach...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00695-9

    authors： Takadoi M,Yamaguchi K,Terashima S

    更新日期：2002-11-18 00:00:00

  • Powerful probes for glycosidases: novel, fluorescently tagged glycosidase inhibitors.

    abstract：:Amino-1,2,5-trideoxy-2,5-imino-D-mannitol was fluorescently tagged by reaction with dansyl chloride at N-1 or by attachment of a dansyl amide bearing spacer to this centre. Compounds obtained are highly potent inhibitors of beta-glucosidase exhibiting Ki values in the single figure nanomolar range. The 1-N-dansyl subs...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00209-8

    authors： Hermetter A,Scholze H,Stütz AE,Withers SG,Wrodnigg TM

    更新日期：2001-05-21 00:00:00

  • Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.04.017

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

    更新日期：2014-06-01 00:00:00

  • Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

    abstract：:Discovery of a new class of DFG-out p38α kinase inhibitors with no hinge interaction is described. A computationally assisted, virtual fragment-based drug design (vFBDD) platform was utilized to identify novel non-aromatic fragments which make productive hydrogen bond interactions with Arg 70 on the αC-helix. Molecule...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.09.078

    authors： Moffett K,Konteatis Z,Nguyen D,Shetty R,Ludington J,Fujimoto T,Lee KJ,Chai X,Namboodiri H,Karpusas M,Dorsey B,Guarnieri F,Bukhtiyarova M,Springman E,Michelotti E

    更新日期：2011-12-01 00:00:00

  • Wortmannilactones I-L, new NADH-fumarate reductase inhibitors, induced by adding suberoylanilide hydroxamic acid to the culture medium of Talaromyces wortmannii.

    abstract：:With the aim of finding more potential inhibitors against NADH-fumarate reductase (specific target for treating helminthiasis and cancer) from natural resources, Talaromyces wortmannii was treated with the epigenome regulatory agent suberoylanilide hydroxamic acid, which resulted in the isolation of four new wortmanni...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.09.032

    authors： Liu WC,Wang YY,Liu JH,Ke AB,Zheng ZH,Lu XH,Luan YS,Xiu ZL,Dong YS

    更新日期：2016-11-01 00:00:00

  • Synthesis of 2-methyl-1,4-naphthoquinones with higher gamma-glutamyl carboxylase activity than MK-4 both in vitro and in vivo.

    abstract：:Vitamin K is the collective term for compounds that share a 2-methyl-1,4-naphthoquinone ring, but differ in the side-chain at the 3-position. We synthesized novel 2-methyl-1,4-naphthoquinone derivatives with different side chain length at the 3-position. Derivatives with C-14 and C-16 tails showed the highest in vitro...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.11.073

    authors： Vermeer C,van 't Hoofd C,Knapen MHJ,Xanthoulea S

    更新日期：2017-01-15 00:00:00

  • Flavonoids: structural requirements for antiproliferative activity on breast cancer cells.

    abstract：:Several classes of flavonoids (flavones, flavanones, 2'-hydroxychalcones and flavan-4-ols) having a variety of substituents on A ring were investigated for their antiproliferative activity against MCF-7 human breast cancer cells. Structure-activity relationships of these compounds were discussed. 2'-hydroxychalcones a...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00617-5

    authors： Pouget C,Lauthier F,Simon A,Fagnere C,Basly JP,Delage C,Chulia AJ

    更新日期：2001-12-17 00:00:00

  • Novel cytokine release inhibitors. Part II: Steroids.

    abstract：:Steroidal derivatives as IL-1 beta release inhibitors are discussed. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(98)00521-6

    authors： He W,Huang FC,Morytko M,Jariwala N,Yu KT

    更新日期：1998-10-20 00:00:00

  • N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists.

    abstract：:A series of 1-adamantanecarboxamides was synthesized and examined for their potency as a selective 5-HT2 receptor antagonist. We found (S)-N-[1-[2-(4-fluorophenyl)ethyl]pyrrolidin-3-yl]-1-adamantane carboxamide hydrochloride hydrate (10-(S), Y-39241) to have a high affinity and selectivity for 5-HT2 receptors, and thi...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00492-3

    authors： Fujio M,Kuroita T,Sakai Y,Nakagawa H,Matsumoto Y

    更新日期：2000-11-06 00:00:00

  • Synthesis, absolute configuration and antimuscarinic activity of the enantiomers of [1-(2,2-diphenyl-[1,3]dioxolan-4-yl)-ethyl]-dimethyl-amine.

    abstract：:Methylation of the carbon atom C of compound 1, a potent and not selective muscarinic antagonist, was carried out. The resulting diastereomers were separated and the corresponding racemate further resolved to give four enantiomers, which were tested both as hydrogen oxalate and methiodide salts. The pharmacological re...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00647-8

    authors： Gulini U,Angeli P,Marucci G,Buccioni M,Giardinà D,Antolini L,Franchini S,Sorbi C,Brasili L

    更新日期：2001-01-22 00:00:00

  • Novel quinolizidine salicylamide influenza fusion inhibitors.

    abstract：:A novel series of quinolizidine salicylamides was synthesized as specific inhibitors of the H1 subtype of influenza A viruses. These inhibitors inhibit the pH-induced fusion process, thereby blocking viral entry into host cells. Compound 16 was the most active inhibitor in this series with an EC50 of 0.25 microg/mL in...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00361-3

    authors： Yu KL,Ruediger E,Luo G,Cianci C,Danetz S,Tiley L,Trehan AK,Monkovic I,Pearce B,Martel A,Krystal M,Meanwell NA

    更新日期：1999-08-02 00:00:00

  • Identification of fragments targeting an alternative pocket on HIV-1 gp41 by NMR screening and similarity searching.

    abstract：:The HIV-1 envelope glycoprotein gp41 fusion intermediate is a promising drug target for inhibiting viral entry. However, drug development has been impeded by challenges inherent in mediating the underlying protein-protein interaction. Here we report on the identification of fragments that bind to a C-terminal sub-pock...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.07.026

    authors： Chu S,Gochin M

    更新日期：2013-09-15 00:00:00

  • Chemo-enzymatic synthesis of imidazolium-tagged sialyllactosamine probes.

    abstract：:Two novel α-linked sialyltrisaccharide imidazolium-type probes (ITags) based on the structures of biologically relevant 6'-sialyllactosamine and 3'-sialyllactosamine were efficiently and stereoselectively prepared using a chemo-enzymatic approach. The apparent kinetic parameters for the enzyme catalyzed transformation...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.07.049

    authors： Sittel I,Galan MC

    更新日期：2015-10-01 00:00:00

  • Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.

    abstract：:The synthesis and biological profile of a novel series of potent and selective inhibitors of cysteine protease cathepsin K (Cat K) are described. Pharmacokinetic evaluation of 12 indicated that some members of this series could be suitable candidates to develop new orally active therapeutic agents for the treatment of...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.05.061

    authors： Setti EL,Venkatraman S,Palmer JT,Xie X,Cheung H,Yu W,Wesolowski G,Robichaud J

    更新日期：2006-08-15 00:00:00

  • Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells.

    abstract：:A benzopyranopyridine inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MK2) is prepared rapidly and efficiently in one step using microwave dielectric heating, whereas a substrate-selective p38 MAPK inhibitor was prepared using conventional heating techniques. The former had MK2 inhibitory act...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.10.036

    authors： Davis T,Bagley MC,Dix MC,Murziani PG,Rokicki MJ,Widdowson CS,Zayed JM,Bachler MA,Kipling D

    更新日期：2007-12-15 00:00:00

  • Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.

    abstract：:A series of indene analogs of the H(1)-antihistamine (-)-R-dimethindene was evaluated for selectivity in the search for potentially improved sedative-hypnotics. Variation of the 6-substitutent in the indene core in combination with a pendant electron rich heterocycle led to the identification of several potent H(1)-an...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.02.055

    authors： Li BF,Moree WJ,Yu J,Coon T,Zamani-Kord S,Malany S,Jalali K,Wen J,Wang H,Yang C,Hoare SR,Petroski RE,Madan A,Crowe PD,Beaton G

    更新日期：2010-04-15 00:00:00

  • Lobelane analogues containing 4-hydroxy and 4-(2-fluoroethoxy) aromatic substituents: Potent and selective inhibitors of [(3)H]dopamine uptake at the vesicular monoamine transporter-2.

    abstract：:A series of lobelane and GZ-793A analogues that incorporate aromatic 4-hydroxy and 4-(2-fluoroethoxy) substituents were synthesized and evaluated for inhibition of [(3)H]dopamine (DA) uptake at the vesicular monoamine transporter-2 (VMAT2) and the dopamine transporter (DAT), and [(3)H]serotonin uptake at the serotonin...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.03.119

    authors： Joolakanti SR,Nickell JR,Janganati V,Zheng G,Dwoskin LP,Crooks PA

    更新日期：2016-05-15 00:00:00

  • Design and synthesis of positional isomers of 5 and 6-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles as possible antimicrobial and antitubercular agents.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.06.072

    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

  • Inhibitory effect of carboxylic acid group on hERG binding.

    abstract：:Drug-induced QT prolongation arising from drugs' blocking of hERG channel activity presents significant challenges in drug development. Many, but not all, of our benzamidine-containing factor Xa inhibitors were found to have high hERG binding propensity. However, incorporation of a carboxylic acid group into these ben...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.08.039

    authors： Zhu BY,Jia ZJ,Zhang P,Su T,Huang W,Goldman E,Tumas D,Kadambi V,Eddy P,Sinha U,Scarborough RM,Song Y

    更新日期：2006-11-01 00:00:00

  • Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.

    abstract：:A series of benzotriazole phenyldifluoromethylphosphonic acids were found to be potent PTP-1B inhibitors. Molecular modeling on the X-ray crystal structure of the lead structure led to the design of potent PTP-1B inhibitors that show moderate selectivity against TC-PTP, a very closely related protein tyrosine phosphat...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2003.11.076

    authors： Lau CK,Bayly CI,Gauthier JY,Li CS,Therien M,Asante-Appiah E,Cromlish W,Boie Y,Forghani F,Desmarais S,Wang Q,Skorey K,Waddleton D,Payette P,Ramachandran C,Kennedy BP,Scapin G

    更新日期：2004-02-23 00:00:00

  • Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.

    abstract：:A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various amide modifications and substitution on the left side phenyl ring were prepared and found to show significant inhibitory activities towards both CXCR2 and CXCR1 receptors. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.05.049

    authors： Aki C,Chao J,Ferreira JA,Dwyer MP,Yu Y,Chao J,Merritt RJ,Lai G,Wu M,Hipkin RW,Fan X,Gonsiorek W,Fosseta J,Rindgen D,Fine J,Lundell D,Taveras AG,Biju P

    更新日期：2009-08-01 00:00:00

  • Thiol-based angiotensin-converting enzyme 2 inhibitors: P1 modifications for the exploration of the S1 subsite.

    abstract：:Screening of a metalloprotease library led to the identification of a thiol-based dual ACE/NEP inhibitor as a potent ACE2 inhibitor. Modifications of the P(1) benzyl moiety led to improvements in ACE2 potency as well as to increased selectivity versus ACE and NEP. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.11.048

    authors： Deaton DN,Gao EN,Graham KP,Gross JW,Miller AB,Strelow JM

    更新日期：2008-01-15 00:00:00

  • Enantioselective synthesis of (R)-(+)- and (S)-(-)-higenamine and their analogues with effects on platelet aggregation and experimental animal model of disseminated intravascular coagulation.

    abstract：:Optically active tetrahydroisoquinoline alkaloids, (R)-(+)-higenamine (1R) and (S)-(-)-higenamine (1 S), and their optically active 1-naphthylmethyl analogues (2 and 3), were synthesized by enantioselective hydrogenation of the corresponding dihydroisoquinoline intermediates 7 as a key step. The evaluation of the plat...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.05.094

    authors： Pyo MK,Lee DH,Kim DH,Lee JH,Moon JC,Chang KC,Yun-Choi HS

    更新日期：2008-07-15 00:00:00

  • Antibody-catalyzed cleavage of the D-Ala-D-Lac depsipeptide: an immunological approach to the problem of vancomycin resistance.

    abstract：:Vancomycin resistance is currently a major healthcare problem. The development of a catalytic monoclonal antibody (mAb) that hydrolyzes the D-Ala-D-Lac depsipeptide provides a potentially novel antibiotic strategy. A phosphonate hapten design was used to program antibody catalysis. The characteristics of the hapten we...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00047-1

    authors： Isomura S,Ashley JA,Wirsching P,Janda KD

    更新日期：2002-03-25 00:00:00

  • Further constituents of Galianthe thalictroides (Rubiaceae) and inhibition of DNA topoisomerases I and IIα by its cytotoxic β-carboline alkaloids.

    abstract：:A new cytotoxic β-carboline alkaloid, 1-methyl-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (1), was isolated from roots of Galianthe thalictroides, together with the alkaloid 1-(hydroxymethyl)-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (2), the anthraquinones 1-...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.01.039

    authors： de Oliveira Figueiredo P,Perdomo RT,Garcez FR,de Fatima Cepa Matos M,de Carvalho JE,Garcez WS

    更新日期：2014-03-01 00:00:00

  • Synthesis and evaluation of imidazo[1,5-a]pyrazines as corticotropin releasing hormone receptor ligands.

    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

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00741-7

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

    更新日期：2002-02-11 00:00:00

  • Structure-based lead identification of ATP-competitive MK2 inhibitors.

    abstract：:MK2 kinase is a promising drug discovery target for the treatment of inflammatory diseases. Here, we describe the discovery of novel MK2 inhibitors using X-ray crystallography and structure-based drug design. The lead has in vivo efficacy in a short-term preclinical model. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.04.018

    authors： Barf T,Kaptein A,de Wilde S,van der Heijden R,van Someren R,Demont D,Schultz-Fademrecht C,Versteegh J,van Zeeland M,Seegers N,Kazemier B,van de Kar B,van Hoek M,de Roos J,Klop H,Smeets R,Hofstra C,Hornberg J,Oubrie A

    更新日期：2011-06-15 00:00:00

  • Novel ROS-activated agents utilize a tethered amine to selectively target acute myeloid leukemia.

    abstract：:This study explores the possible use of reactive oxygen-activated DNA modifying agents against acute myeloid leukemia (AML). A key amine on the lead agent was investigated via cytotoxicity assays and was found necessary for potency. The two best compounds were screened via the NCI-60 cell panel. These two compounds ha...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.03.048

    authors： Bell-Horwath TR,Vadukoot AK,Thowfeik FS,Li G,Wunderlich M,Mulloy JC,Merino EJ

    更新日期：2013-05-15 00:00:00

  • 4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.

    abstract：:The first examples of thioether-substituted benzonitriles as potential soft-drug androgen receptor antagonists are reported. A number of 4-(alkylthio)- and of 4-(arylthio)-benzonitrile analogs were evaluated in human androgen receptor binding and cellular functional assays. Analogs with potent in vitro binding and cel...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.01.063

    authors： Mitchell L,Wang Z,Hu LY,Kostlan C,Carroll M,Dettling D,Du D,Pocalyko D,Wade K

    更新日期：2009-03-01 00:00:00

  • O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.

    abstract：:A new class of O-arylmandelic acid PPAR agonists show excellent anti-hyperglycemic efficacy in a db/db mouse model of DM2. These PPARalpha-weighted agonists do not show the typical PPARgamma associated side effects of BAT proliferation and cardiac hypertrophy in a rat tolerability assay. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(03)00702-9

    authors： Adams AD,Hu Z,von Langen D,Dadiz A,Elbrecht A,MacNaul KL,Berger JP,Zhou G,Doebber TW,Meurer R,Forrest MJ,Moller DE,Jones AB

    更新日期：2003-10-06 00:00:00