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Research in pharmaceutical science has become nowadays a major societal challenge as it puts the patient at the forefront of its concerns. This comes along with considerable financial investments and long-term involvement. Accordingly the most innovative technologies are made available to this endeavor. To this end, the progresses in organic chemistry allow for the synthesis of high-quality compound libraries based on the concept of druggability, those library are then employed in the context of high trough-put screening (HTS), a methodology used for the discovery of patentable NCE’s (new chemical entity), some of them will subsequently be marketed. Virtual screening represents also a major breakthrough as it permits to limit the chemical space to be explored and the correlative number of expensive biological tests to be experimentally performed. In this work, initially, the different types of chemical reaction sequences and their significance in the context of multi-component reactions (MCR) are presented. Various examples are shown starting form early MCR applications such as the Strecker reactions till the more contemporary Ugi reaction. In a second part, HTS methodologies are described in a contextual association with MCR approaches La recherche dans le domaine pharmaceutique est un enjeu de société important car elle place le patient au centre de ses préoccupations. Elle s’accompagne d’un investissement financier considérable et d’un engagement sur le long terme. Il est indispensable de mettre à sa disposition les techniques les plus innovantes possibles pour progresser dans la découverte tout en assurant une diminution des coûts pour la production de composés. Pour y parvenir, les progrès réalisés en chimie organique vont permettre la création de chimiothèques de grande qualité basées sur le concept de la druggability. Les librairies moléculaires vont pouvoir être utilisées dans le cadre du screening à haut débit, ce qui va nous permettre de découvrir des nouvelles entités chimiques intéressantes qui devront être développées pour l’obtention de l’autorisation de la mise sur le marché du médicament. Un travail de docking informatique, qui représente des tests de screening virtuel, peut être réalisé au préalable pour limiter la mise en place des tests expérimentaux, très onéreux. Malgré tout la technologie mise en place, le screening à haut débit connaît une stagnation de ses résultats due à divers problèmes notamment l’affinité peu élevée des composés obtenus envers leurs cibles. La future décennie sera primordiale pour l’avancée des tests de screening. Nous présenterons tout d’abord, les différents types de réactions chimiques existants. Nous expliquerons les différents paramètres de la réaction multi-composante. Divers exemples seront illustrés et ce, à partir du 19ème siècle avec Strecker jusqu’à nos jours. Ensuite, nous passerons à l’étude de la chimiothèque sous tous ses aspects ainsi que l’application de la réaction d’Ugi à ce concept. Enfin, nous terminerons par le criblage à haut débit qui est une technique de pointe s’associant parfaitement à l’utilisation des chimiothèques.

Small Molecules libraries --- Drug Industry

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This eBook is a collection of articles from a Frontiers Research Topic. Frontiers Research Topics are very popular trademarks of the Frontiers Journals Series: they are collections of at least ten articles, all centered on a particular subject. With their unique mix of varied contributions from Original Research to Review Articles, Frontiers Research Topics unify the most influential researchers, the latest key findings and historical advances in a hot research area! Find out more on how to host your own Frontiers Research Topic or contribute to one as an author by contacting the Frontiers Editorial Office: frontiersin.org/about/contact

Medicine --- Oncology --- Cancer --- Target --- Small Molecules --- Antibodies --- Therapy

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This eBook is a collection of articles from a Frontiers Research Topic. Frontiers Research Topics are very popular trademarks of the Frontiers Journals Series: they are collections of at least ten articles, all centered on a particular subject. With their unique mix of varied contributions from Original Research to Review Articles, Frontiers Research Topics unify the most influential researchers, the latest key findings and historical advances in a hot research area! Find out more on how to host your own Frontiers Research Topic or contribute to one as an author by contacting the Frontiers Editorial Office: frontiersin.org/about/contact

Medicine --- Oncology --- Cancer --- Target --- Small Molecules --- Antibodies --- Therapy

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• Reference Manager
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• RefWorks (Direct export to RefWorks)

This eBook is a collection of articles from a Frontiers Research Topic. Frontiers Research Topics are very popular trademarks of the Frontiers Journals Series: they are collections of at least ten articles, all centered on a particular subject. With their unique mix of varied contributions from Original Research to Review Articles, Frontiers Research Topics unify the most influential researchers, the latest key findings and historical advances in a hot research area! Find out more on how to host your own Frontiers Research Topic or contribute to one as an author by contacting the Frontiers Editorial Office: frontiersin.org/about/contact

cancer stem cells (CSC) --- therapeutic targeting --- antibodies --- transcription factors --- small molecules

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This eBook is a collection of articles from a Frontiers Research Topic. Frontiers Research Topics are very popular trademarks of the Frontiers Journals Series: they are collections of at least ten articles, all centered on a particular subject. With their unique mix of varied contributions from Original Research to Review Articles, Frontiers Research Topics unify the most influential researchers, the latest key findings and historical advances in a hot research area! Find out more on how to host your own Frontiers Research Topic or contribute to one as an author by contacting the Frontiers Editorial Office: frontiersin.org/about/contact

Medicine --- Oncology --- cancer stem cells (CSC) --- therapeutic targeting --- antibodies --- transcription factors --- small molecules