A5075406067- Melanoma and MAPK Pathways
- Synthesis and biological activity
- Computational Drug Discovery Methods
- Cancer Mechanisms and Therapy
- Quinazolinone synthesis and applications
- Cancer therapeutics and mechanisms
- Biochemical and Molecular Research
- Synthesis of heterocyclic compounds
- Cytokine Signaling Pathways and Interactions
- Synthesis and Biological Evaluation
- Synthesis of Tetrazole Derivatives
Korea University of Science and Technology
2019-2023
Korea Institute of Science and Technology
2019-2023
Modern University for Information and Technology
2022-2023
BRAF is an important component of MAPK cascade. Mutation BRAF, in particular V600E, leads to hyperactivation the pathway and uncontrolled cellular growth. Resistance selective inhibitors mutated a major obstacle against treatment many cancer types. In this work, series new (imidazo[2,1-b]thiazol-5-yl)pyrimidine derivatives possessing terminal sulfonamide moiety were synthesized. Pan-RAF inhibitory effect was investigated, structure–activity relationship discussed. Antiproliferative activity...
In the current article, we introduce design of a new series 4-(imidazol-5-yl)pyridines with improved anticancer activity and selective B-RAFV600E/p38α kinase inhibitory activity. Based on previous work, group structural modifications were applied affording potential antiproliferative agents. Towards extensive biological assessment target compounds, an in vitro assay was conducted over NCI 60-cancer cell lines panel representing blood, lung, colon, CNS, skin, ovary, renal, prostate, breast...
A series of 36 pyrazol-4yl pyridine derivatives (8a-i, 9a-i, 10a-i, and 11a-i ) was designed, synthesized, evaluated for its antiproliferative activity over NCI-60 cancer cell line panel inhibitory effect against JNK isoforms (JNK1, JNK2, JNK3). All the synthesized compounds were tested panel. Compounds 11b, 11c, 11g, 11i selected to determine their GI50s exerted a superior potency than reference standard SP600125 lines. 11c showed GI50 1.28 μM K562 leukemic cells. Vero cells used assess...