Discovery of 5‐(2‐(Phenylamino)pyrimidin‐4‐yl)thiazol‐2(3H)‐one Derivatives as Potent Mnk2 Inhibitors: Synthesis, SAR Analysis and Biological Evaluation

…, M Kumarasiri, P Li, M Yu, F Lam, SKC Basnet… - …, 2014 - Wiley Online Library
Phosphorylation of eIF4E by human mitogen‐activated protein kinase (MAPK)‐interacting
kinases (Mnks) is crucial for human tumourigenesis and development. Targeting Mnks may …

Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug …

…, MH Rahaman, B Noll, SKC Basnet… - Journal of Medicinal …, 2017 - ACS Publications
Cyclin D dependent kinases (CDK4 and CDK6) regulate entry into S phase of the cell cycle
and are validated targets for anticancer drug discovery. Herein we detail the discovery of a …

Discovery of 4-(dihydropyridinon-3-yl) amino-5-methylthieno [2, 3-d] pyrimidine derivatives as potent Mnk inhibitors: synthesis, structure–activity relationship analysis …

M Yu, P Li, SKC Basnet, M Kumarasiri, S Diab… - European journal of …, 2015 - Elsevier
Phosphorylation of the eukaryotic initiation factor 4E (eIF4E) by mitogen-activated protein
kinase (MAPK)-interacting kinases (Mnks) is essential for oncogenesis but unnecessary for …

Pharmacologic inhibition of MNKs in acute myeloid leukemia

T Teo, F Lam, M Yu, Y Yang, SKC Basnet… - Molecular …, 2015 - ASPET
The Ras/Raf/MAPK and PI3K/Akt/mTOR pathways are key signaling cascades involved in the
regulation of cell proliferation and survival, and have been implicated in the pathogenesis …

Discovery of CDK5 inhibitors through structure-guided approach

…, S Tadesse, M Kumarasiri, SKC Basnet… - ACS Medicinal …, 2019 - ACS Publications
Specific abrogation of cyclin-dependent kinase 5 (CDK5) activity has been validated as a
viable approach for the development of anticancer agents. However, no selective CDK5 …

Dual Inhibition of Mnk2 and FLT3 for potential treatment of acute myeloid leukaemia

S Diab, AM Abdelaziz, P Li, T Teo, SKC Basnet… - European Journal of …, 2017 - Elsevier
The discovery of novel anti-AML therapeutic agents is urgently needed, but the complex
heterogeneity of the disease has so far hampered the development of a curative treatment. FLT3 …

[HTML][HTML] An orally bioavailable and highly efficacious inhibitor of cdk9/flt3 for the treatment of acute myeloid leukemia

…, Y Long, G Heinemann, J Karanjia, B Noll, SKC Basnet… - Cancers, 2022 - mdpi.com
Simple Summary CDDD11-8 is an orally bioactive pharmacological inhibitor of CDK9. In
AML cells, CDDD11-8 suppressed the proliferation and caused robust inhibition of tumor …

2-Anilino-4-(1-methyl-1H-pyrazol-4-yl) pyrimidine-derived CDK2 inhibitors as anticancer agents: Design, synthesis & evaluation

BS Fanta, L Mekonnen, SKC Basnet, T Teo… - Bioorganic & Medicinal …, 2023 - Elsevier
Deregulation of cyclin-dependent kinase 2 (CDK2) and its activating partners, cyclins A and
E, is associated with the pathogenesis of a myriad of human cancers and with resistance to …

An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis

T Teo, Y Yang, M Yu, SKC Basnet, T Gillam… - European journal of …, 2015 - Elsevier
Deregulation of protein synthesis is a common event in cancer. As MAPK-interacting kinases
(Mnks) play critical roles in regulation of protein synthesis, they have emerged as novel anti-…

[HTML][HTML] Inhibition of Mnk enhances apoptotic activity of cytarabine in acute myeloid leukemia cells

P Li, S Diab, M Yu, J Adams, S Islam, SKC Basnet… - Oncotarget, 2016 - ncbi.nlm.nih.gov
Cytarabine (Ara-C) is a first line clinical therapeutic agent for treatment of acute myeloid
leukemia (AML). However, this therapy is limited due to high rate of resistance and relapse. …