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Special Issue "Recent Advances in Diversity-Oriented Synthesis"

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A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Molecular Diversity".

Deadline for manuscript submissions: closed (31 August 2014)

Special Issue Editor

Guest Editor
Dr. Eamon Comer

Broad Institute of MIT and Harvard, 7 Cambridge Center Cambridge, MA, 02142, USA
Interests: diversity oriented synthesis; medicinal chemistry; drug discovery; chemical technology; infectious diseases

Special Issue Information

Dear Colleagues,

Historically, small-molecule screening collections have tended to be heavily populated with achiral, aromatic compounds that can be prepared efficiently and at low cost, but which occupy a narrow region of chemical space. These collections have led to major contributions to our drug pharmacopeia, but have not produced useful leads for numerous targets. This failure has led to the outlook that we may not be able to find pharmaceuticals for such targets.

However, we have recently witnessed the emergence of many innovative strategies for the assembly of chemically diverse libraries that cover a much broader region of chemical space. Diversity-oriented synthesis offers a systematic and efficient strategy to synthesize collections of structurally complex and functionally diverse small molecules that may ultimately exert their biological effects through unique mechanisms. DOS libraries have various common features, such as an increased ratio of sp3-hybridized atoms and a greater number of stereogenic elements relative to conventional compound libraries. These collections combine the structural complexity of natural products with the efficiency of high-throughput synthesis. These new diverse molecular scaffolds are leading to remarkable advances in chemistry and biology.

For this Special Issue, we invite the submission of manuscripts focusing on current investigations in the field of DOS, such as the development and evaluation of new synthetic strategies and approaches, and the application of these diverse molecular scaffolds in probing new biology.

Dr. Eamon Comer
Guest Editor

Submission

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. Papers will be published continuously (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are refereed through a peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed Open Access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs).


Keywords

  • diversity-oriented synthesis
  • asymmetric synthesis
  • next generation synthesis
  • stereodivergence and stereoselectivity
  • chemical library synthesis
  • probe molecules
  • biologically active molecules
  • drug discovery
  • molecular scaffolds

Published Papers (2 papers)

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Review

Open AccessReview Diversity-Oriented Synthetic Strategies Applied to Cancer Chemical Biology and Drug Discovery
Molecules 2014, 19(11), 17221-17255; doi:10.3390/molecules191117221
Received: 22 August 2014 / Revised: 13 October 2014 / Accepted: 17 October 2014 / Published: 27 October 2014
Cited by 7 | PDF Full-text (1654 KB) | HTML Full-text | XML Full-text
Abstract
How can diversity-oriented strategies for chemical synthesis provide chemical tools to help shape our understanding of complex cancer pathways and progress anti-cancer drug discovery efforts? This review (surveying the literature from 2003 to the present) considers the applications of diversity-oriented synthesis (DOS), [...] Read more.
How can diversity-oriented strategies for chemical synthesis provide chemical tools to help shape our understanding of complex cancer pathways and progress anti-cancer drug discovery efforts? This review (surveying the literature from 2003 to the present) considers the applications of diversity-oriented synthesis (DOS), biology-oriented synthesis (BIOS) and associated strategies to cancer biology and drug discovery, summarising the syntheses of novel and often highly complex scaffolds from pluripotent or synthetically versatile building blocks. We highlight the role of diversity-oriented synthetic strategies in producing new chemical tools to interrogate cancer biology pathways through the assembly of relevant libraries and their application to phenotypic and biochemical screens. The use of diversity-oriented strategies to explore structure-activity relationships in more advanced drug discovery projects is discussed. We show how considering appropriate and variable focus in library design has provided a spectrum of DOS approaches relevant at all stages in anti-cancer drug discovery. Full article
(This article belongs to the Special Issue Recent Advances in Diversity-Oriented Synthesis)
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Open AccessReview Diversity-Oriented Synthesis as a Tool for Chemical Genetics
Molecules 2014, 19(10), 16506-16528; doi:10.3390/molecules191016506
Received: 22 August 2014 / Revised: 30 September 2014 / Accepted: 1 October 2014 / Published: 14 October 2014
Cited by 6 | PDF Full-text (1488 KB) | HTML Full-text | XML Full-text
Abstract
Chemical genetics is an approach for identifying small molecules with the ability to induce a biological phenotype or to interact with a particular gene product, and it is an emerging tool for lead generation in drug discovery. Accordingly, there is a need [...] Read more.
Chemical genetics is an approach for identifying small molecules with the ability to induce a biological phenotype or to interact with a particular gene product, and it is an emerging tool for lead generation in drug discovery. Accordingly, there is a need for efficient and versatile synthetic processes capable of generating complex and diverse molecular libraries, and Diversity-Oriented Synthesis (DOS) of small molecules is the concept of choice to give access to new chemotypes with high chemical diversity. In this review, the combination of chemical genetics and diversity-oriented synthesis to identify new chemotypes as hit compounds in chemical biology and drug discovery is reported, giving an overview of basic concepts and selected case studies. Full article
(This article belongs to the Special Issue Recent Advances in Diversity-Oriented Synthesis)
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