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Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.
TLDR
Molecular modeling indicated that interaction of this scaffold with Asp186 and Lys67 residues within the ATP-binding pocket might be responsible for the kinase inhibitory potency.
Synthesis and evaluation of the antiproliferative activity of novel thiazoloquinazolinone kinases inhibitors
The microwave-assisted synthesis of a family of 2,8-substituted thiazoloquinazolinones is described. The preliminary evaluation of the antiproliferative activity and the capacity of these molecules
Synthesis of novel 5-substituted indirubins as protein kinases inhibitors.
TLDR
In an effort to identify new pharmacological inhibitors of disease-relevant protein kinases with increased potency and selectivity, new 5-substituted indirubin derivatives were synthesized and evaluated.
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and
TLDR
Combination of lead optimization and molecular modeling studies allowed identification of a dual CDK1/GSK-3 inhibitor (compound 13d) with submicromolar values.
Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors.
TLDR
Several compounds appear to be particularly promising for the development of tools in the battle against Alzheimer's disease, as well as the subfamily CLK2-3.
A one-pot synthesis and biological activity of ageladine A and analogues.
TLDR
The key Pictet-Spengler reaction between 2-aminohistamine and aryl aldehydes has been successfully utilized for the synthesis of the natural product and 14 analogues, creating the first structure-activity relationship of ageladine A analogues.
Thiazolo[5,4-f]quinazolin-9-ones, inhibitors of glycogen synthase kinase-3.
TLDR
Molecular modeling studies suggest that the most selective GSK-3 inhibitors 7a-d bind into the ATP-binding site through a key hydrogen bond interaction with Val135 and target the specific hydrophobic backpocket of the enzyme.
Antitumoral effects of cyclin-dependent kinases inhibitors CR8 and MR4 on chronic myeloid leukemia cell lines
TLDR
This study investigates ability of CR8 isomers and MR4, three derivatives of the cyclin-dependent kinases (CDKs) inhibitor Roscovitine, to exert anti-leukemic activities against chronic myeloid leukemia in vitro and then deciphers their mechanisms of action.
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