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MORE KUNAL NANDKUMAR,장동조,Jun-Young Lee,Jeong-Hoon Park 대한방사성의약품학회 2019 Journal of radiopharmaceuticals and molecular prob Vol.5 No.1
Hypoxia-inducible factor-1 (HIF-1α) is a transcription factor activated in response to low oxygen level, and ishighly expressed in many solid tumors. Moreover, HIF-1α is a representative biomarker of hypoxia and alsohelps to maintain cell homeostasis under hypoxic condition. Most solid tumors show hypoxia, which inducespoor prognosis and resistance to conventional cancer therapies. Thus, early diagnosis of hypoxia with positronemission tomography (PET) radiotracer would be highly beneficial for management of malignant solid tumorswith effective cancer therapy. YC-1 is a most promising candidate among several HIF-1α inhibitors. As an effortto develop a hypoxia imaging tool as a PET radiotracer, we designed and synthesized [18F]DFYC based onpotent derivative of YC-1 and performed preliminary in vitro cell uptake study. [18F]DFYC showed a significantaccumulation in SKBR-3 cells among other cancer cells, proving as a good lead to develop a hypoxic solidtumor such as breast cancer.
MORE KUNAL NANDKUMAR,이진호 대한화학회 2017 Bulletin of the Korean Chemical Society Vol.38 No.1
Angiogenesis is critical for tumor growth and mediated mainly by vascular endothelial growth factor (VEGF) signaling. Inhibition of the VEGF signaling pathway has emerged as one of the promising approaches for cancer therapy. VEGF receptor 2 (VEGFR-2) is considered as a major mediator of angiogenic effects of VEGF. We describe herein the discovery of a series of potent VEGFR-2 tyrosine kinase (KDR) inhibitors from a new 2-(2-aminopyrimidin-4-yl)phenol scaffold. The KDR activity was reduced appreciably by a series of compounds with a benzoyl group at position 4 of phenol ring. The structure–activity relationships for a series of (3-(2-aminopyrimidin-4-yl)-4-hydroxyphenyl)phenyl methanones revealed compound 9 (KDR IC50 = 25 nM) as the most potent inhibitor in the series. Compound 22 had a potent cellular activity on VEGF-induced HUVEC cell growth (IC50 < 0.1 μM) with high selectivity over HCT116.
이진호,MORE KUNAL NANDKUMAR,양선아,Victor S. Hong 대한화학회 2014 Bulletin of the Korean Chemical Society Vol.35 No.7
Pim kinases are promising targets in the treatment of hematopoietic and solid cancers. Meridianin C was chosen as a starting point to discover novel pim kinase inhibitors. Using known pim kinase’s structural information, aminopyrimidine was introduced to provide the hydrogen-bonding interactions with the conserved lysine residue in the ATP binding pocket of all three Pim kinases. Synthesized 3,5-bis(aminopyrimidinyl)indole derivatives showed pan-pim inhibitory activity. Aminoalkyl substituent was attached on the aminopyrimidine to further enhance the potency and physicochemical properties of compound. The research reveals a significative way of designing compounds with high potency and kinase selectivity for pan-pim kinases.