Pyrimidine: a review on anticancer activity with key emphasis on SAR

A Mahapatra, T Prasad, T Sharma - Future journal of pharmaceutical …, 2021 - Springer
Background Cancer is a global health challenge, it impacts the quality of life and its
treatment is associated with several side effects. Resistance of the cancer cells to the …

Recent developments in anticancer kinase inhibitors based on the pyrazolo [3, 4-d] pyrimidine scaffold

DJ Baillache, A Unciti-Broceta - RSC medicinal chemistry, 2020 - pubs.rsc.org
Pyrazolo [3, 4-d] pyrimidines have become of significant interest for the medicinal chemistry
community as a privileged scaffold for the development of kinase inhibitors to treat a range …

Synthesis of 4, 6-disubstituted pyrazolo [3, 4-d] pyrimidine analogues: Cyclin-dependent kinase 2 (CDK2) inhibition, molecular docking and anticancer evaluation

S Cherukupalli, B Chandrasekaran, RR Aleti… - Journal of Molecular …, 2019 - Elsevier
The cyclin-dependent kinases (CDKs) play a crucial role in cell cycle progression and are
validated targets of cancer therapy. Pyrazolopyrimidines are versatile scaffolds, which have …

A New Strategy for Glioblastoma Treatment: In Vitro and In Vivo Preclinical Characterization of Si306, a Pyrazolo[3,4-d]Pyrimidine Dual Src/P-Glycoprotein Inhibitor

AL Fallacara, C Zamperini, A Podolski-Renić, J Dinić… - Cancers, 2019 - mdpi.com
Overexpression of P-glycoprotein (P-gp) and other ATP-binding cassette (ABC) transporters
in multidrug resistant (MDR) cancer cells is responsible for the reduction of intracellular drug …

Novel pyrazolo [3, 4-d] pyrimidines as dual Src/Bcr-Abl kinase inhibitors: synthesis and biological evaluation for chronic myeloid leukemia treatment

S Di Maria, F Picarazzi, M Mori, A Cianciusi… - Bioorganic …, 2022 - Elsevier
Abstract The Bcr-Abl tyrosine kinase (TK) is the molecular hallmark of chronic myeloid
leukemia (CML). Src is another TK kinase whose involvement in CML was widely …

Biological Evaluation and In Vitro Characterization of ADME Profile of In-House Pyrazolo[3,4-d]pyrimidines as Dual Tyrosine Kinase Inhibitors Active against …

F Poggialini, C Vagaggini, A Brai, C Pasqualini… - Pharmaceutics, 2023 - mdpi.com
The therapeutic use of tyrosine kinase inhibitors (TKIs) represents one of the successful
strategies for the treatment of glioblastoma (GBM). Pyrazolo [3, 4-d] pyrimidines have …

A comprehensive review on the indazole based derivatives as targeted anticancer agents

S Puri, S Sawant, K Juvale - Journal of Molecular Structure, 2023 - Elsevier
Cancer is one of the leading causes of death worldwide, resulting in the deaths of millions of
individuals. Owing to the development of drug resistance to conventional therapies …

Prodrugs of Pyrazolo[3,4-d]pyrimidines: From Library Synthesis to Evaluation as Potential Anticancer Agents in an Orthotopic Glioblastoma Model

G Vignaroli, G Iovenitti, C Zamperini… - Journal of Medicinal …, 2017 - ACS Publications
Pyrazolo [3, 4-d] pyrimidines are potent protein kinase inhibitors with promising antitumor
activity but suboptimal aqueous solubility, consequently worth being further optimized …

Development of Pyrazolo[3,4-d]pyrimidine Kinase Inhibitors as Potential Clinical Candidates for Glioblastoma Multiforme

C Greco, V Taresco, AK Pearce, CE Vasey… - ACS Medicinal …, 2020 - ACS Publications
Glioblastoma multiforme (GBM) is the most aggressive primary brain tumor. Residual cells at
the tumor margin are responsible for up to 85% of GBM recurrences after standard …

Studies on the ATP binding site of Fyn kinase for the identification of new inhibitors and their evaluation as potential agents against tauopathies and tumors

C Tintori, G La Sala, G Vignaroli, L Botta… - Journal of Medicinal …, 2015 - ACS Publications
Fyn is a member of the Src-family of nonreceptor protein–tyrosine kinases. Its abnormal
activity has been shown to be related to various human cancers as well as to severe …