Current Fragment-to-lead Approaches Starting from the 7-azaindole: The Pharmacological Versatility of a Privileged Molecular Fragment

Author:

Marcos Santos Leandro12ORCID,da Silveira Nelson José Freitas1

Affiliation:

1. Laboratory of Molecular Modeling and Computer Simulation / MolMod-CS (D311-F), Institute of Chemistry, Federal University of Alfenas / UNIFAL-MG, Alfenas, Minas Gerais, 37130-001, Brazil

2. Pharmaceutical Chemistry Research Laboratory / LQFar (D202A), Department of Food and Medicines, Faculty of Pharmaceutical Sciences, Federal University of Alfenas / UNIFAL-MG, Alfenas, Minas Gerais, 37130-001, Brazil

Abstract

Abstract: Fragment-based drug discovery is one of the most powerful paradigms in the recent context of medicinal chemistry and is being widely practiced by academic and industrial researchers. Currently, azaindoles are among the most exploited molecular fragments in pharmaceutical innovation projects inspired by fragment-to-lead strategies. The 7-azaindole is the most prominent representative within this remarkable family of pyrrolopyridine fragments, as it is present in the chemical structure of several approved antitumor drugs and also of numerous therapeutic candidates. In this paper, a brief overview on existing proofs of concept in the literature will be presented, as well as some recent works that corroborate 7-azaindole as a privileged and pharmacologically versatile molecular fragment.

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,General Medicine

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