Benzimidazole‐oxindole hybrids: A novel class of selective dual CDK2 and GSK‐3β inhibitors of potent anticancer activity
Sign Up to like & getrecommendations! Published in 2024 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202300721
Abstract: A new series of benzimidazole‐oxindole hybrids 8a–x was discovered as dual cyclin‐dependent kinase (CDK2) and glycogen synthase kinase‐3‐beta (GSK‐3β) inhibitors with potent anticancer activity. The synthesized hits displayed potent anticancer activity against national cancer institute… read more here.
Keywords: cdk2; cdk2 gsk; benzimidazole oxindole; potent anticancer ... See more keywords
Molecular docking and MD simulation studies of 4-thiazol-N-(pyridin-2-yl)pyrimidin-2-amine derivatives as novel inhibitors targeted to CDK2/4/6
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Cancer Research and Clinical Oncology"
DOI: 10.1007/s00432-024-05818-y
Abstract: Nowadays, cyclin-dependent kinase 4/6 (CDK4/6) inhibitors have been approved for treating metastatic breast cancer and have achieved inspiring curative effects. But some discoveries have indicated that CDK 4/6 are not the requisite factors in some… read more here.
Keywords: molecular docking; cdk2 inhibitors; cdk2; amine derivatives ... See more keywords
Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112322
Abstract: In the current study, we have designed and synthesized a series of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent kinase2 (CDK2) dual inhibitors by integrating purine-based pharmacophore into the recognition cap group of CS055. The representative… read more here.
Keywords: novel histone; cyclin dependent; cdk2; hdac1 cyclin ... See more keywords
Synthesis, characterization and in-silico assessment of novel thiazolidinone derivatives for cyclin-dependent kinases-2 inhibitors
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Molecular Structure"
DOI: 10.1016/j.molstruc.2020.129311
Abstract: Abstract This work aims to synthesize thiazolidinone derivatives using a rapid, safe and solvent-free grinding assisted approach. The newly synthesized compounds have been targeted due to their bioactivity in wide pharmaceutical uses, especially, as anti-proliferative… read more here.
Keywords: cyclin dependent; synthesis characterization; thiazolidinone derivatives; characterization silico ... See more keywords
Screening through Lead Optimization of High Affinity, Allosteric Cyclin-Dependent Kinase 2 (CDK2) Inhibitors as Male Contraceptives That Reduce Sperm Counts in Mice.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01731
Abstract: Although cyclin-dependent kinase 2 (CDK2) is a validated target for both cancer and contraception, developing a CDK2 inhibitor with exquisite selectivity has been challenging due to the structural similarity of the ATP-binding site, where most… read more here.
Keywords: cdk2; dependent kinase; affinity; cyclin dependent ... See more keywords
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b00663
Abstract: In the present study, a novel series of 3-pyrimidinylazaindoles were designed and synthesized using a bioinformatics strategy as cyclin-dependent kinases CDK2 and CDK9 inhibitors, which play critical roles in the cell cycle control and regulation… read more here.
Keywords: negative breast; vivo; cdk2; breast cancer ... See more keywords
Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2062337
Abstract: Abstract In the current work, a hybridisation strategy was adopted between the privileged building blocks, benzofuran and piperazine, with the aim of designing novel CDK2 type II inhibitors. The hybrid structures were linked to different… read more here.
Keywords: cell; identification piperazinylmethyl; cdk2; benzofuran derivatives ... See more keywords
PolyC-binding proteins enhance expression of the CDK2 cell cycle regulatory protein via alternative splicing
Sign Up to like & getrecommendations! Published in 2018 at "Nucleic Acids Research"
DOI: 10.1093/nar/gkx1255
Abstract: Abstract The PolyC binding proteins (PCBPs) impact alternative splicing of a subset of mammalian genes that are enriched in basic cellular functions. Here, we focus our analysis on PCBP-controlled cassette exon-splicing within the cell cycle… read more here.
Keywords: polyc binding; alternative splicing; cdk2; cell cycle ... See more keywords
Repression of Mafb promotes foreskin fibroblast proliferation through upregulation of CDK2, cyclin E and PCNA
Sign Up to like & getrecommendations! Published in 2022 at "Andrologia"
DOI: 10.1111/and.14411
Abstract: Mafb plays a significant role in the development and differentiation of various organs, tissues and cells. Nevertheless, its role in the control of external genital cell proliferation and function in the mechanism of hypospadias remains… read more here.
Keywords: pcna; cdk2; proliferation; mafb ... See more keywords
CDK2 positively regulates aerobic glycolysis by suppressing SIRT5 in gastric cancer
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Science"
DOI: 10.1111/cas.13691
Abstract: Although significant progress has been made in the diagnosis and treatment of gastric cancer, the overall survival rate of the disease remains unchanged at approximately 20%‐25%. Thus, there is an urgent need for a better… read more here.
Keywords: gastric cancer; cell metabolism; cdk2; cancer cell ... See more keywords
Aconitate decarboxylase 1 is a mediator of polymicrobial sepsis
Sign Up to like & getrecommendations! Published in 2022 at "Science Translational Medicine"
DOI: 10.1126/scitranslmed.abo2028
Abstract: Sepsis is a challenging clinical syndrome caused by a dysregulated host response to infection. Here, we identified an unexpected proseptic activity of aconitate decarboxylase 1 (ACOD1) in monocytes and macrophages. Previous studies have suggested that… read more here.
Keywords: sepsis; cdk2; aconitate decarboxylase; polymicrobial sepsis ... See more keywords