Hepatocellular carcinoma (HCC) is one of the most fatal cancer types worldwide. HCC cells were proved to overexpress c-Src and Sgk1, a tyrosine and a serine-threonine kinase, respectively, whose role is crucial for the development and progression of the tumor. Pyrazolo[3,4-d]pyrimidine derivatives are a class of tyrosine kinase inhibitors that...
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2018 (v1)PublicationUploaded on: April 14, 2023
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2017 (v1)Publication
Pyrazolo[3,4-d]pyrimidine derivatives 1–5, active as c-Src inhibitors, have been selected to be formulated as drug-loaded human serum albumin (HSA) nanoparticles, with the aim of improving their solubility and pharmacokinetic properties. The present study includes the optimization of a desolvation method-based procedure for preparing HSA...
Uploaded on: April 14, 2023 -
2016 (v1)Publication
Pyrazolo[3,4-d]pyrimidines are a class of compounds with a good activity against several cancer cell lines. Despite the promising anticancer activity, these molecules showed a poor aqueous solubility. This issue could threat the future development of pyrazolo[3,4-d]pyrimidines as clinical drug candidates. With the aim of improving their...
Uploaded on: April 14, 2023 -
2023 (v1)Publication
The abnormal activation of Src family kinases (SFKs) due to deregulation of the B-cell receptor (BCR) signalling pathway provides a promising target for development of new pharmacological strategy to overcome the ibrutinib resistance in diffuse large B-cell lymphoma (DLBCL). In this work, we demonstrated that Si409, a...
Uploaded on: July 3, 2024 -
2017 (v1)Publication
Pyrazolo[3,4-d]pyrimidines are potent protein kinase inhibitors with promising antitumor activity but suboptimal aqueous solubility, consequently worth being further optimized. Herein, we present the one-pot two-step procedure for the synthesis of a set of pyrazolo[3,4-d]pyrimidine prodrugs (1a-8a and 9a-e) with higher aqueous solubility and...
Uploaded on: April 14, 2023 -
2015 (v1)Publication
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 pathologies, such as Alzheimer's and Parkinson's diseases. Herein, a structure-based drug design protocol was employed aimed at identifying novel Fyn inhibitors. Two hits...
Uploaded on: April 14, 2023