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  1. AU="Millemaggi, Alessia"
  2. AU=Paulsen Paige
  3. AU="Fan, Su-Su"
  4. AU="de Azeredo, Andressa Cardoso"
  5. AU="Miller, Russell"
  6. AU="A Mombet"

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  1. Article ; Online: The renaissance of alpha-methylene-gamma-butyrolactones: new synthetic approaches.

    Kitson, Russell R A / Millemaggi, Alessia / Taylor, Richard J K

    Angewandte Chemie (International ed. in English)

    2009  Volume 48, Issue 50, Page(s) 9426–9451

    Abstract: The amount of research activity concerning alpha-methylene-gamma-butyrolactones and alpha-alkylidene-gamma-butyrolactones has increased dramatically in recent years. This Review summarizes the structural types, biological activities, and biosynthesis of ... ...

    Abstract The amount of research activity concerning alpha-methylene-gamma-butyrolactones and alpha-alkylidene-gamma-butyrolactones has increased dramatically in recent years. This Review summarizes the structural types, biological activities, and biosynthesis of these compounds, concentrating on publications from the past 10 years. Traditional approaches to alpha-methylene-gamma-butyrolactones and alpha-alkylidene-gamma-butyrolactones are then reviewed together with novel approaches, including those from our own research group, reported more recently.
    MeSH term(s) 4-Butyrolactone/analogs & derivatives ; 4-Butyrolactone/biosynthesis ; 4-Butyrolactone/chemical synthesis ; 4-Butyrolactone/therapeutic use ; Drug Evaluation, Preclinical ; Molecular Structure ; Structure-Activity Relationship
    Chemical Substances alpha-methylene gamma-butyrolactone (362Y256BOL) ; 4-Butyrolactone (OL659KIY4X)
    Language English
    Publishing date 2009-11-20
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.200903108
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: The Renaissance of α-Methylene-γ-butyrolactones: New Synthetic Approaches

    Kitson, Russell R.A / Millemaggi, Alessia / Taylor, Richard J.K

    Angewandte Chemie. 2009 Dec. 07, v. 48, no. 50

    2009  

    Abstract: The amount of research activity concerning α-methylene-γ-butyrolactones and α-alkylidene-γ-butyrolactones has increased dramatically in recent years. This Review summarizes the structural types, biological activities, and biosynthesis of these compounds, ...

    Abstract The amount of research activity concerning α-methylene-γ-butyrolactones and α-alkylidene-γ-butyrolactones has increased dramatically in recent years. This Review summarizes the structural types, biological activities, and biosynthesis of these compounds, concentrating on publications from the past 10 years. Traditional approaches to α-methylene-γ-butyrolactones and α-alkylidene-γ-butyrolactones are then reviewed together with novel approaches, including those from our own research group, reported more recently.
    Language English
    Dates of publication 2009-1207
    Size p. 9426-9451.
    Publishing place Wiley-VCH Verlag
    Document type Article
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.200903108
    Database NAL-Catalogue (AGRICOLA)

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  3. Article ; Online: A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).

    Johnson, Christopher N / Ahn, Jong Sook / Buck, Ildiko M / Chiarparin, Elisabetta / Day, James E H / Hopkins, Anna / Howard, Steven / Lewis, Edward J / Martins, Vanessa / Millemaggi, Alessia / Munck, Joanne M / Page, Lee W / Peakman, Torren / Reader, Michael / Rich, Sharna J / Saxty, Gordon / Smyth, Tomoko / Thompson, Neil T / Ward, George A /
    Williams, Pamela A / Wilsher, Nicola E / Chessari, Gianni

    Journal of medicinal chemistry

    2018  Volume 61, Issue 16, Page(s) 7314–7329

    Abstract: Inhibitor of apoptosis proteins (IAPs) are promising anticancer targets, given their roles in the evasion of apoptosis. Several peptidomimetic IAP antagonists, with inherent selectivity for cellular IAP (cIAP) over X-linked IAP (XIAP), have been tested ... ...

    Abstract Inhibitor of apoptosis proteins (IAPs) are promising anticancer targets, given their roles in the evasion of apoptosis. Several peptidomimetic IAP antagonists, with inherent selectivity for cellular IAP (cIAP) over X-linked IAP (XIAP), have been tested in the clinic. A fragment screening approach followed by structure-based optimization has previously been reported that resulted in a low-nanomolar cIAP1 and XIAP antagonist lead molecule with a more balanced cIAP-XIAP profile. We now report the further structure-guided optimization of the lead, with a view to improving the metabolic stability and cardiac safety profile, to give the nonpeptidomimetic antagonist clinical candidate 27 (ASTX660), currently being tested in a phase 1/2 clinical trial (NCT02503423).
    MeSH term(s) Administration, Oral ; Animals ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacokinetics ; Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Crystallography, X-Ray ; ERG1 Potassium Channel/antagonists & inhibitors ; Heterocyclic Compounds, 2-Ring/chemistry ; Heterocyclic Compounds, 2-Ring/pharmacokinetics ; Heterocyclic Compounds, 2-Ring/pharmacology ; Humans ; Inhibitor of Apoptosis Proteins/antagonists & inhibitors ; Macaca fascicularis ; Male ; Mice, Inbred BALB C ; Piperazines/chemistry ; Piperazines/pharmacokinetics ; Piperazines/pharmacology ; Rats, Sprague-Dawley ; Structure-Activity Relationship ; X-Linked Inhibitor of Apoptosis Protein/antagonists & inhibitors ; X-Linked Inhibitor of Apoptosis Protein/chemistry ; X-Linked Inhibitor of Apoptosis Protein/metabolism ; Xenograft Model Antitumor Assays
    Chemical Substances AT-IAP compound ; Antineoplastic Agents ; ERG1 Potassium Channel ; Heterocyclic Compounds, 2-Ring ; Inhibitor of Apoptosis Proteins ; KCNH2 protein, human ; Piperazines ; X-Linked Inhibitor of Apoptosis Protein ; XIAP protein, human
    Language English
    Publishing date 2018-08-09
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.8b00900
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
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    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

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  4. Article ; Online: Complete deracemization by attrition-enhanced ostwald ripening elucidated.

    Noorduin, Wim L / Meekes, Hugo / van Enckevort, Willem J P / Millemaggi, Alessia / Leeman, Michel / Kaptein, Bernard / Kellogg, Richard M / Vlieg, Elias

    Angewandte Chemie (International ed. in English)

    2008  Volume 47, Issue 34, Page(s) 6445–6447

    MeSH term(s) Amides/chemistry ; Amides/isolation & purification ; Amino Acids/chemistry ; Amino Acids/isolation & purification ; Benzyl Compounds/chemistry ; Benzyl Compounds/isolation & purification ; Chemical Fractionation ; Crystallization ; Glycine/analogs & derivatives ; Glycine/chemistry ; Glycine/isolation & purification ; Stereoisomerism
    Chemical Substances Amides ; Amino Acids ; Benzyl Compounds ; N-(2-methylbenzylidene)-phenylglycine amide ; Glycine (TE7660XO1C)
    Language English
    Publishing date 2008
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.200801846
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  5. Article: Complete Deracemization by Attrition-Enhanced Ostwald Ripening Elucidated

    Noorduin, Wim L / Meekes, Hugo / van Enckevort, Willem J.P / Millemaggi, Alessia / Leeman, Michel / Kaptein, Bernard / Kellogg, Richard M / Vlieg, Elias

    Angewandte Chemie. 2008 Aug. 11, v. 47, no. 34

    2008  

    Language English
    Dates of publication 2008-0811
    Size p. 6445-6447.
    Publishing place Wiley-VCH Verlag
    Document type Article
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.200801846
    Database NAL-Catalogue (AGRICOLA)

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  6. Article: EuFOD-Catalyzed Hetero-Diels-Alder (HDA) Reaction under Microwave Heating

    Panunzio, Mauro / Bandini, Elisa / D’Aurizio, Antonio / Millemaggi, Alessia / Xia, Zhining

    Synthesis

    2007  Volume 2007, Issue 13, Page(s) 2060–2062

    Abstract: An efficient EuFOD-catalyzed hetero-Diels-Alder reaction between azadienes and aldehydes under microwave irradiation is reported. The reaction proceeds under microwave heating with 5 mol% of EuFOD in 45-83% yields. ...

    Abstract An efficient EuFOD-catalyzed hetero-Diels-Alder reaction between azadienes and aldehydes under microwave irradiation is reported. The reaction proceeds under microwave heating with 5 mol% of EuFOD in 45-83% yields.
    Keywords azadiene ; Diels-Alder reaction ; lactams ; lanthanides ; amino alcohols
    Language English
    Publishing date 2007-03-12
    Publishing place Stuttgart ; New York
    Document type Article
    ZDB-ID 2033062-5
    ISSN 1437-210X ; 0039-7881
    ISSN (online) 1437-210X
    ISSN 0039-7881
    DOI 10.1055/s-2007-965985
    Database Thieme publisher's database

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  7. Article ; Online: Emergence of a single solid chiral state from a nearly racemic amino acid derivative.

    Noorduin, Wim L / Izumi, Toshiko / Millemaggi, Alessia / Leeman, Michel / Meekes, Hugo / Van Enckevort, Willem J P / Kellogg, Richard M / Kaptein, Bernard / Vlieg, Elias / Blackmond, Donna G

    Journal of the American Chemical Society

    2008  Volume 130, Issue 4, Page(s) 1158–1159

    MeSH term(s) Amino Acids/chemistry ; Biochemistry/methods ; Chemistry/methods ; Chemistry, Physical/methods ; Crystallization ; Kinetics ; Models, Chemical ; Pharmaceutical Preparations/chemical synthesis ; Salts/chemistry ; Stereoisomerism ; Thermodynamics
    Chemical Substances Amino Acids ; Pharmaceutical Preparations ; Salts
    Language English
    Publishing date 2008-01-30
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/ja7106349
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Bonn / Germany

    Z 4' 55/32: Show issues
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