Pyrrolopyrimidine derivatives represent a class of biologically active heterocyclic compounds which can serve as promising scaffolds that display remarkable biological activities, such as anti-inflammatory, antimicrobial, antiviral and anticancer. In the last few years, several pyrrolopyrimidine derivatives have been approved by the US FDA and in other countries for the treatment of different diseases or are currently in phase I/II clinical trials. Due to their inimitable antioxidant and anti-tumor properties, researchers were inspired to develop novel derivatives for the treatment of different types of cancer. The present review summarizes recent literature up to 2017 on the most recent development in the medicinal chemistry of pyrrolopyrimidine derivatives and their potential as anticancer therapeutics, especially compounds acting as kinase inhibitors.
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Identification of a series of pyrrolo-pyrimidine based SARS-CoV-2 Mac1 inhibitors that repress coronavirus replication.
bioRxiv
October 2024
Department of Molecular Biosciences, University of Kansas, Lawrence, Kansas, USA.
Article Synopsis
- Coronaviruses can originate from animals and cause serious illnesses in both humans and animals, with a key protein called Mac1 playing a role in viral replication and interferon inhibition.
- Researchers discovered a compound, MCD-628, that inhibits Mac1 but found its effectiveness was limited due to poor permeability.
- By creating more hydrophobic derivatives, they identified four compounds that successfully inhibited Mac1 and reduced replication of coronaviruses, confirming their specificity through drug-resistance mutations, but this resistance came at a cost to the virus's overall fitness.
Amide Functionalized Novel Pyrrolo-pyrimidine Derivative as Anticancer Agents: Synthesis, Characterization and Molecular Docking Studies.
Anticancer Agents Med Chem
November 2024
Department of Chemistry, Andhra University, Vishakhapatnam, Andhra Pradesh.
Background: The development of new therapies targeting crucial kinases involved in cancer progression is a promising area of research. Pyrazolo pyrimidine derivatives have emerged as potential candidates for this purpose.
Objective: This study aims to synthesize pyrazolo pyrimidine derivatives (5a-5r), evaluate their molecular docking against key kinases, and assess their anticancer activity.
Pyrrolo[2,3-d]pyrimidines as potential kinase inhibitors in cancer drug discovery: A critical review.
Bioorg Chem
December 2024
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India. Electronic address:
Pyrrolo[2,3-d]pyrimidine-based kinase inhibitors have emerged as an important class of targeted therapeutics to combat various types of cancer. The distinctive structural feature of pyrrolopyrimidine ring system offers an adaptable platform for designing potent inhibitors of various kinases, crucial in regulating cellular processes. The deazapurine framework inherent to pyrrolopyrimidines bears a conspicuous resemblance to adenine, the natural ligand ATP.
View Article and Find Full Text PDFExperimental and computational evaluation of anti-malarial and antioxidant potential of transition metal (II) complexes with tridentate schiff base derived from pyrrolopyrimidine.
Biometals
December 2024
Department of Pharmacology, Saveetha Dental College and Hospital, Saveetha Institute of Medical and Technical Sciences, Chennai, Tamil Nadu, 600077, India.
Article Synopsis
- The 21st century has seen increasing variations of pathogens, leading to significant global health issues, particularly malaria and oxidative damage, which necessitate the search for effective treatments.* -
- Research is focused on the antioxidant potential of transition metal (II) complexes with tridentate Schiff base ligands, as they might enhance both anti-malarial and antioxidant activities, offering a two-fold therapeutic benefit.* -
- Investigations into various metal complexes showed that some, particularly the Hg(II) complex, exhibit strong anti-malarial properties similar to quinine, while Cu(II) and Zn(II) complexes demonstrate significant antioxidant capabilities, supported by molecular docking studies to assess their pharmacological interactions.*
Synthesis, Evaluation and Docking Studies of Disubstituted N-Heterocyclic Derivatives as Anticancer Agents.
Chem Biodivers
December 2024
Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Shoolini University, Solan, H.P., 173 229, India.
Cancer is a chronic disease reported with alarming rates of mortalities every year. Herein, we reported the synthesis of nitrogen based novel heterocyclic disubstituted derivatives and evaluated them against L929 and A549 cell lines using MTT assay. Among all, 6a2 and 6c1 were significantly active against L929 with IC value of 2.
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