Sunita K. C. Basnet
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View article: A brain-penetrant CDK4/6 inhibitor - AU3-14 shows robust anti-tumor efficacy against glioblastoma
A brain-penetrant CDK4/6 inhibitor - AU3-14 shows robust anti-tumor efficacy against glioblastoma Open
The cyclin D-CDK4/6-INK4-Rb pathway is frequently dysregulated in glioblastoma (GBM), the most aggressive and poorly prognosed brain malignancy. Despite extensive research, advances in GBM treatment have seen limited progress, with current…
View article: A novel CDK4 inhibitor for myeloid protection in chemotherapy-treated triple-negative breast Cancer
A novel CDK4 inhibitor for myeloid protection in chemotherapy-treated triple-negative breast Cancer Open
Summary Background Despite advances in cancer treatment, chemotherapy remains a cornerstone of clinical practice. However, its efficacy is often compromised by dose-limiting haematologic toxicities. Recent strategies aim to enhance chemoth…
View article: Discovery of N,4-Di(1H-pyrazol-4-yl)pyrimidin-2-amine-Derived CDK2 Inhibitors as Potential Anticancer Agents: Design, Synthesis, and Evaluation
Discovery of N,4-Di(1H-pyrazol-4-yl)pyrimidin-2-amine-Derived CDK2 Inhibitors as Potential Anticancer Agents: Design, Synthesis, and Evaluation Open
Cyclin-dependent kinase 2 (CDK2) has been garnering considerable interest as a target to develop new cancer treatments and to ameliorate resistance to CDK4/6 inhibitors. However, a selective CDK2 inhibitor has yet to be clinically approved…
View article: 2-Anilino-4-(1-methyl-1H-pyrazol-4-yl)pyrimidine-derived CDK2 inhibitors as anticancer agents: Design, synthesis & evaluation
2-Anilino-4-(1-methyl-1H-pyrazol-4-yl)pyrimidine-derived CDK2 inhibitors as anticancer agents: Design, synthesis & evaluation Open
View article: An Orally Bioavailable and Highly Efficacious Inhibitor of CDK9/FLT3 for the Treatment of Acute Myeloid Leukemia
An Orally Bioavailable and Highly Efficacious Inhibitor of CDK9/FLT3 for the Treatment of Acute Myeloid Leukemia Open
Mutations in FMS-like tyrosine kinase 3 (FLT3) occur in approximately one-third of AML patients and are associated with a particularly poor prognosis. The most common mutation, FLT3-ITD, is a self-activating internal tandem duplication (IT…
View article: Discovery of Novel and Potent Inhibitors of Cyclin-Dependent Kinases 7 and 9: Design, Synthesis, Structure-Activity Relationship Analysis and Biological Evaluation
Discovery of Novel and Potent Inhibitors of Cyclin-Dependent Kinases 7 and 9: Design, Synthesis, Structure-Activity Relationship Analysis and Biological Evaluation Open
View article: Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations Open
View article: Synthesis and evaluation of 2′H-spiro[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione derivatives as Mnk inhibitors
Synthesis and evaluation of 2′H-spiro[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione derivatives as Mnk inhibitors Open
View article: Discovery of CDK5 Inhibitors through Structure-Guided Approach
Discovery of CDK5 Inhibitors through Structure-Guided Approach Open
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 inhibitor has been reported to date. Herein, a structure-based
View article: Dual Inhibition of Mnk2 and FLT3 for potential treatment of acute myeloid leukaemia
Dual Inhibition of Mnk2 and FLT3 for potential treatment of acute myeloid leukaemia Open
View article: Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-<i>N</i>-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation
Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-<i>N</i>-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation Open
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 novel series of 4-thiazol-N-(pyridin-2-yl)pyrimidin-2-ami…
View article: Inhibition of Mnk enhances apoptotic activity of cytarabine in acute myeloid leukemia cells
Inhibition of Mnk enhances apoptotic activity of cytarabine in acute myeloid leukemia cells Open
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. Recent research has revealed that the poor prognosis …
View article: An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis Open
View article: Discovery of 4-(dihydropyridinon-3-yl)amino-5-methylthieno[2,3-d]pyrimidine derivatives as potent Mnk inhibitors: synthesis, structure–activity relationship analysis and biological evaluation
Discovery of 4-(dihydropyridinon-3-yl)amino-5-methylthieno[2,3-d]pyrimidine derivatives as potent Mnk inhibitors: synthesis, structure–activity relationship analysis and biological evaluation Open