Affiliation:
1. Department of Chemistry, Faculty of Science, Helwan University, Cairo 11795, Egypt
2. Department of Pharmaceutical Chemistry,
Faculty of Pharmacy, Helwan University, Cairo 11795, Egypt
3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy,
Kuwait University, Kuwait
4. Department of Medicinal Chemistry, Egyptian Ministry of Health and Population, Cairo, Egypt
Abstract
Background:
Medicinal chemistry of pyrazolopyrimidine scaffolds substituted with different heterocyclic
nuclei has attracted great attention due to their wide range of biological activities that have been reported.
Pyrazolopyrimidine scaffold is an important privileged heterocycle nucleus in drug discovery.
Methods:
All pharmacological activities of pyrazolopyrimidine scaffold have been mentioned, such as anticancer,
anti-inflammatory, antihypertensive, antitubercular, antiviral, antibacterial, antifungal, antidiabetic, and
anti-obesity agents. In addition, it was used in both osteoporosis and neurological disorders. The difference in
potency and bioavailability of pyrazolopyrimidine derivatives refers to the substituent groups that can increase
the activity against specific targets and enhance their selectivity.
Results:
This review provides an overview of different synthetic pathways, structure activity relationships, and
preclinical studies of pyrazolopyrimidine scaffolds substituted with a variety of heterocyclic nuclei, as well as it
provides a discussion on the significant biological findings of these important scaffolds. In addition, it provides
some insights on the different macromolecular targets that pyrazolopyrimidine scaffold can effectively work on,
such as; cyclin dependent kinases; CDK2, CDK7, and CDK9, checkpoint kinases; CHK1 and CHK2 and their
correlation with the anticancer activity, PI3Kα, transient receptor potential canonical 6, B-Raf kinase, Interleukin-
1 receptor-associated kinase 4, B-cell lymphoma 6, TRKA-C kinase, potent kDa ribosomal protein S6
kinase, colon cancer cell line (CaCo-2), domain receptor kinase (KDR), HepG-2 carcinoma cell, FLT3. The antibacterial
activity against B. subtilis and E. coli and antifungal activity against C. albicans, C. tropicalis,
A. niger, and A. clavatus are discussed.
Conclusion:
This review provides an overview of the different pharmacological activities of the pyrazolopyrimidine
scaffold and its correlation with chemical structure. Some exciting new developments in pyrazolopyrimidine
scaffolds are also presented in this review.
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmacology
Cited by
3 articles.
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