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  1. Article: Profile. K. C. Nicolaou.

    Nicolaou, K C

    Organic & biomolecular chemistry

    2003  Volume 1, Issue 6, Page(s) x–xi

    Language English
    Publishing date 2003-03-21
    Publishing country England
    Document type Interview
    ZDB-ID 2097583-1
    ISSN 1477-0539 ; 1477-0520
    ISSN (online) 1477-0539
    ISSN 1477-0520
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Corrigendum: The Role of Organic Synthesis in the Emergence and Development of Antibody-Drug Conjugates as Targeted Cancer Therapies.

    Nicolaou, K C / Rigol, Stephan

    Angewandte Chemie (International ed. in English)

    2021  Volume 60, Issue 32, Page(s) 17246–17247

    Language English
    Publishing date 2021-07-27
    Publishing country Germany
    Document type Published Erratum
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.202108147
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  3. Article ; Online: Total Synthesis of Apoptolidin: Part 2. Coupling of Key Building Blocks and Completion of the Synthesis We thank Dr. C. Khosla and Dr. Y. Hayakawa for generous gifts of apoptolidin, and Dr. D. H. Huang and Dr. G. Siuzdak for NMR spectroscopic and mass spectrometric assistance, respectively. This work was financially supported by the National Institutes of Health (USA), the Skaggs Institute for Chemical Biology, American Biosciences, a predoctoral fellowship from Boehringer Ingelheim (to Y.L.), a postdoctoral fellowship the George Hewitt Foundation (to K.C.F.), and grants from Abbott Laboratories, ArrayBiopharma, Bayer, Boehringer Ingelheim, DuPont, Glaxo, Hoffmann-LaRoche, Merck, Novartis, Pfizer, and Schering Plough.

    Nicolaou, K. C. / Li, Yiwei / Fylaktakidou, Konstantina C. / Mitchell, Helen J. / Sugita, Kazuyuki

    Angewandte Chemie (International ed. in English)

    2001  Volume 40, Issue 20, Page(s) 3854–3857

    Language English
    Publishing date 2001-10-15
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
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  4. Article ; Online: Total Synthesis of Apoptolidin: Part 1. Retrosynthetic Analysis and Construction of Building Blocks We thank Dr. D. H. Huang and Dr. G. Siuzdak for NMR spectroscopic and mass spectrometric assistance, respectively. This work was financially supported by the National Institutes of Health (USA), the Skaggs Institute for Chemical Biology, American Biosciences, a pre-doctoral fellowship from Boehringer Ingelheim (Y.L.), a postdoctoral fellowship the George Hewitt Foundation (K.C.F.), and grants from Abbott Laboratories, ArrayBiopharma, Bayer, Boehringer Ingelheim, DuPont, Glaxo, Hoffmann-LaRoche, Merck, Novartis, Pfizer, and Schering Plough.

    Nicolaou, K. C. / Li, Yiwei / Fylaktakidou, Konstantina C. / Mitchell, Helen J. / Wei, Heng-Xu / Weyershausen, Bernd

    Angewandte Chemie (International ed. in English)

    2001  Volume 40, Issue 20, Page(s) 3849–3854

    Language English
    Publishing date 2001-10-15
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Perspectives from nearly five decades of total synthesis of natural products and their analogues for biology and medicine.

    Nicolaou, K C / Rigol, Stephan

    Natural product reports

    2020  Volume 37, Issue 11, Page(s) 1404–1435

    Abstract: Covering: 1970 to 2020By definition total synthesis is the art and science of making the molecules of living Nature in the laboratory, and by extension, their analogues. Although obvious, its application to the synthesis of molecules for biology and ... ...

    Abstract Covering: 1970 to 2020By definition total synthesis is the art and science of making the molecules of living Nature in the laboratory, and by extension, their analogues. Although obvious, its application to the synthesis of molecules for biology and medicine was not always the purpose of total synthesis. In recent years, however, the field has acquired momentum as its power to reach higher molecular complexity and diversity is increasing, and as the demand for rare bioactive natural products and their analogues is expanding due to their recognised potential to facilitate biology and drug discovery and development. Today this component of total synthesis endeavors is considered highly desirable, and could be part of interdisciplinary academic and/or industrial partnerships, providing further inspiration and momentum to the field. In this review we provide a brief historical background of the emergence of the field of total synthesis as it relates to making molecules for biology and medicine. We then discuss specific examples of this practice from our laboratories as they developed over the years. The review ends with a conclusion and future perspectives for natural products chemistry and its applications to biology and medicine and other added-value contributions to science and society.
    MeSH term(s) Biological Products/chemical synthesis ; Biological Products/chemistry ; Biological Products/pharmacology ; Drug Discovery ; Molecular Structure
    Chemical Substances Biological Products
    Language English
    Publishing date 2020-04-22
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S. ; Review
    ZDB-ID 2002546-4
    ISSN 1460-4752 ; 0265-0568
    ISSN (online) 1460-4752
    ISSN 0265-0568
    DOI 10.1039/d0np00003e
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article: Perspectives from nearly five decades of total synthesis of natural products and their analogues for biology and medicine

    Nicolaou, K. C. / Rigol, Stephan

    Natural product reports. 2020 Nov. 18, v. 37, no. 11

    2020  

    Abstract: By definition total synthesis is the art and science of making the molecules of living Nature in the laboratory, and by extension, their analogues. Although obvious, its application to the synthesis of molecules for biology and medicine was not always ... ...

    Abstract By definition total synthesis is the art and science of making the molecules of living Nature in the laboratory, and by extension, their analogues. Although obvious, its application to the synthesis of molecules for biology and medicine was not always the purpose of total synthesis. In recent years, however, the field has acquired momentum as its power to reach higher molecular complexity and diversity is increasing, and as the demand for rare bioactive natural products and their analogues is expanding due to their recognised potential to facilitate biology and drug discovery and development. Today this component of total synthesis endeavors is considered highly desirable, and could be part of interdisciplinary academic and/or industrial partnerships, providing further inspiration and momentum to the field. In this review we provide a brief historical background of the emergence of the field of total synthesis as it relates to making molecules for biology and medicine. We then discuss specific examples of this practice from our laboratories as they developed over the years. The review ends with a conclusion and future perspectives for natural products chemistry and its applications to biology and medicine and other added-value contributions to science and society.
    Keywords chemistry ; drugs ; medicine ; momentum
    Language English
    Dates of publication 2020-1118
    Size p. 1404-1435.
    Publishing place The Royal Society of Chemistry
    Document type Article
    ZDB-ID 2002546-4
    ISSN 1460-4752 ; 0265-0568
    ISSN (online) 1460-4752
    ISSN 0265-0568
    DOI 10.1039/d0np00003e
    Database NAL-Catalogue (AGRICOLA)

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  7. Article ; Online: Total Synthesis of Gukulenin B via Sequential Tropolone Functionalizations.

    Nicolaou, K C / Yu, Ruocheng / Lu, Zhaoyong / Alvarez, Fernando G

    Journal of the American Chemical Society

    2022  Volume 144, Issue 11, Page(s) 5190–5196

    Abstract: ... a series of site-selective aromatic C-H bond functionalizations and C-C bond formations, whose reaction ...

    Abstract The synthesis of functionalized aromatic compounds is a central theme of research for modern organic chemistry. Despite the increasing finesse in the functionalization of five- and six-membered aromatic rings, their seven-membered-ring sibling, tropolone (2-hydroxy-2,4,6-cycloheptatrien-1-one), remains a challenging target for synthetic derivatization. This challenge primarily emanates from the unique structural and chemical properties of tropolonoid compounds, which often lead to unexpected and undesired reaction outcomes under conditions developed for the functionalizations of other aromatic moieties. Herein, we describe the total synthesis of one of the most complex natural tropolonoids, gukulenin B. Our synthetic route features a series of site-selective aromatic C-H bond functionalizations and C-C bond formations, whose reaction conditions are judiciously tuned to allow uncompromised performance on the tropolone nucleus. The flexibility and modularity of our synthesis are expected to facilitate further synthetic and biological studies of the gukulenin family of cytotoxins. In addition, the methods and tactics developed herein for the functionalization of the tropolone moiety could inspire and enable chemists of multiple disciplines to take advantage of this privileged yet underexplored structural motif.
    MeSH term(s) Organic Chemicals ; Terpenes ; Tropolone
    Chemical Substances Organic Chemicals ; Terpenes ; gukulenin B ; Tropolone (7L6DL16P1T)
    Language English
    Publishing date 2022-03-11
    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/jacs.2c01305
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: The Role of Organic Synthesis in the Emergence and Development of Antibody-Drug Conjugates as Targeted Cancer Therapies.

    Nicolaou, K C / Rigol, Stephan

    Angewandte Chemie (International ed. in English)

    2019  Volume 58, Issue 33, Page(s) 11206–11241

    Abstract: With a number of antibody-drug conjugates (ADCs) approved for clinical use as targeted cancer therapies and numerous candidates in clinical trials, the field of ADCs is emerging as one of the frontiers in biomedical research, particularly in the area of ... ...

    Abstract With a number of antibody-drug conjugates (ADCs) approved for clinical use as targeted cancer therapies and numerous candidates in clinical trials, the field of ADCs is emerging as one of the frontiers in biomedical research, particularly in the area of cancer treatment. Chemists, biologists and clinicians, among other scientists, are partnering their expertise to improve their design, synthesis, efficacy and precision as they strive to advance this paradigm of personalized and targeted medicine to treat cancer patients more effectively and to expand its scope to other indications. Just as Alexander Fleming's penicillin, and the myriad other bioactive natural products that followed its discovery and success in the clinic, ignited a revolution in medicine after the Second World War, so did calicheamicin γ
    MeSH term(s) Antibodies, Monoclonal/therapeutic use ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/therapeutic use ; Chemistry Techniques, Synthetic/methods ; Drug Delivery Systems ; Humans ; Immunoconjugates/chemistry ; Neoplasms/drug therapy
    Chemical Substances Antibodies, Monoclonal ; Antineoplastic Agents ; Immunoconjugates
    Language English
    Publishing date 2019-07-08
    Publishing country Germany
    Document type Journal Article ; Research Support, N.I.H., Extramural ; 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.201903498
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  9. Article ; Online: Academic-industrial partnerships in drug discovery and development.

    Nicolaou, K C

    Angewandte Chemie (International ed. in English)

    2014  Volume 53, Issue 19, Page(s) 4730–4731

    MeSH term(s) Biological Products/chemistry ; Chemistry, Pharmaceutical ; Drug Discovery ; Interinstitutional Relations
    Chemical Substances Biological Products
    Language English
    Publishing date 2014-05-05
    Publishing country Germany
    Document type Editorial
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.201402816
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  10. Article ; Online: Advancing the drug discovery and development process.

    Nicolaou, K C

    Angewandte Chemie (International ed. in English)

    2014  Volume 53, Issue 35, Page(s) 9128–9140

    Abstract: The current state of affairs in the drug discovery and development process is briefly summarized and then ways to take advantage of the ever-increasing fundamental knowledge and technical knowhow in chemistry and biology and related disciplines are ... ...

    Abstract The current state of affairs in the drug discovery and development process is briefly summarized and then ways to take advantage of the ever-increasing fundamental knowledge and technical knowhow in chemistry and biology and related disciplines are discussed. The primary motivation of this Essay is to celebrate the great achievements of chemistry, biology, and medicine and to inform and inspire students and academics to enter the field of drug discovery and development while, at the same time, continue to advance the fundamentals of their disciplines. It is also meant to encourage and catalyze multidisciplinary partnerships between academia and industry as scientists attempt to merge their often complementary interests and expertise to achieve new improvements and breakthroughs in their respective fields, and the common goal of applying them to the discovery and invention of new and better medicines, especially in areas of unmet needs.
    MeSH term(s) Drug Discovery ; Drug Industry ; Humans
    Language English
    Publishing date 2014-08-25
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S.
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.201404761
    Database MEDical Literature Analysis and Retrieval System OnLINE

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