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      Functional Pyrazolo[1,5- a]pyrimidines: Current Approaches in Synthetic Transformations and Uses As an Antitumor Scaffold

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          Abstract

          Pyrazolo[1,5- a]pyrimidine ( PP) derivatives are an enormous family of N-heterocyclic compounds that possess a high impact in medicinal chemistry and have attracted a great deal of attention in material science recently due to their significant photophysical properties. Consequently, various researchers have developed different synthesis pathways for the preparation and post-functionalization of this functional scaffold. These transformations improve the structural diversity and allow a synergic effect between new synthetic routes and the possible applications of these compounds. This contribution focuses on an overview of the current advances (2015–2021) in the synthesis and functionalization of diverse pyrazolo[1,5- a]pyrimidines. Moreover, the discussion highlights their anticancer potential and enzymatic inhibitory activity, which hopefully could lead to new rational and efficient designs of drugs bearing the pyrazolo[1,5- a]pyrimidine core.

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          Hexafluoroisopropanol as a highly versatile solvent

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            Discovery of Zanubrutinib (BGB-3111), a Novel, Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

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              Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

              Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.
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                Author and article information

                Contributors
                Role: Academic Editor
                Role: Academic Editor
                Journal
                Molecules
                Molecules
                molecules
                Molecules
                MDPI
                1420-3049
                05 May 2021
                May 2021
                : 26
                : 9
                : 2708
                Affiliations
                Bioorganic Compounds Research Group, Department of Chemistry, Universidad de los Andes, Carrera 1 No. 18A-10, Bogotá 111711, Colombia; aj.arias@ 123456uniandes.edu.co (A.A.-G.); af.godoy@ 123456uniandes.edu.co (A.G.)
                Author notes
                [* ]Correspondence: jportill@ 123456uniandes.edu.co ; Tel.: +571-339-4949
                Author information
                https://orcid.org/0000-0002-2196-2204
                https://orcid.org/0000-0002-8206-7481
                Article
                molecules-26-02708
                10.3390/molecules26092708
                8125733
                34063043
                28f29c7f-738b-4f03-8e7a-4a06b9bc8846
                © 2021 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( https://creativecommons.org/licenses/by/4.0/).

                History
                : 23 March 2021
                : 27 April 2021
                Categories
                Review

                antitumor scaffold,enzymatic inhibitory,n-heterocyclic compounds,organic synthesis,pyrazolo[1,5-a]pyrimidine,functionalization

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