A5102840167- PI3K/AKT/mTOR signaling in cancer
- Synthesis and biological activity
- Quinazolinone synthesis and applications
- Click Chemistry and Applications
- Protein Degradation and Inhibitors
- Molecular Sensors and Ion Detection
- Advanced Breast Cancer Therapies
- Nanoplatforms for cancer theranostics
- Chronic Lymphocytic Leukemia Research
- Mast cells and histamine
- Acute Myeloid Leukemia Research
- Cancer Mechanisms and Therapy
- Photodynamic Therapy Research Studies
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Cancer therapeutics and mechanisms
- Advanced biosensing and bioanalysis techniques
- Synthesis and Biological Evaluation
- HER2/EGFR in Cancer Research
- Luminescence and Fluorescent Materials
- Chemotherapy-induced cardiotoxicity and mitigation
- Multiple Myeloma Research and Treatments
- Sulfur Compounds in Biology
- Synthesis of Organic Compounds
- Peptidase Inhibition and Analysis
- Graphene and Nanomaterials Applications
Fudan University
2017-2024
Shenzhen University Health Science Center
2022
Nanyang Technological University
2015
State Key Laboratory of Respiratory Disease
2012
The phosphoinositide 3-kinase (PI3K) inhibitors potently inhibit the signaling pathway of PI3K/AKT/mTOR, which provides a promising new approach for molecularly targeted cancer therapy. In this work, novel series 7-azaindole scaffold derivatives was discovered by fragment-based growing strategy. structure–activity relationship profiles identified that exhibit potent activity against PI3K at molecular and cellular levels as well cell proliferation in panel human tumor cells.
Synthesis and characterization of multifunctional hybrid-polymeric nanoparticles for drug delivery multimodal imaging cancer Danny Jian Hang Tng,1,* Peiyi Song,1,* Guimiao Lin,2,3,* Alana Mauluidy Soehartono,1 Guang Yang,1 Chengbin Feng Yin,1 Cher Heng Tan,4 Ken-Tye Yong1 1School Electrical Electronic Engineering, Nanyang Technological University, Singapore; 2The Engineering Lab Synthetic Biology, 3Research Institute Uropoiesis Reproduction, School Medicine, Shenzhen Shenzhen, People's...
Aberration of PI3K signaling pathway has been confirmed to be associated with several hematological malignancies including acute myeloid leukemia (AML). FD268, a pyridinesulfonamide derivative characterized by the conjugation 7-azaindole group, is newly identified inhibitor showing high potent enzyme activity at nanomole concentration. In this study, we demonstrated that FD268 dose-dependently inhibits survival AML cells efficacy superior PI-103 (pan-PI3K inhibitor) and CAL-101 (selective...
<title>Abstract</title> Considering the common occurrence of adverse cardiovascular events caused by PI3K inhibitors in clinical trials, a comprehensive assessment cardiotoxicity promising inhibitor candidates for their potential translation is great importance. Based on our previous studies 7-azaindazole-based inhibitors, this work, we report novel inhibitor, N-(2-chloro-5-(3-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide (FD274), with low mice. FD274...
Blocking the PI3K and CDK pathways simultaneously has been recognized as a promising strategy for cancer therapy, which may broaden clinical application of or inhibitors. Herein, we report discovery dual PI3K/CDK2 inhibitors utilizing 7-azaindole-based fragment-oriented growth. Among them, compound FD2056 stands out most candidate, maintaining potent inhibitory activity against both CDK2, showing high selectivity among 108 kinases. In cellular assays, inhibitor demonstrated superior...
Despite the recent development of PIM inhibitors based on N-(pyridin-3-yl)acetamide scaffold for acute myeloid leukemia (AML), structural-activity relationship (SAR) associated with effects positional isomerization N toward to Lys67 and freedom solvent fragment Asp128/Glu171 still remains an open question. In this work, a structurally novel compound N-pyridinyl amide was designed by hybridization then our SAR exploration revealed that would lead decrease in activity, while increase breaking...