Novel Quinolinylaminoisoquinoline Bioisosteres of Sorafenib as Selective RAF1 Kinase Inhibitors: Design, Synthesis, and Antiproliferative Activity against Melanoma Cell Line
スポンサーリンク
概要
- 論文の詳細を見る
Design and synthesis of a new series of quinolinylaminoisoquinoline derivatives as conformationally restricted bioisosteres of Sorafenib are described. Their in vitro antiproliferative activity against A375P melanoma cell line was tested. Compounds 1b, 1d, 1g, and 1j showed the highest potency against A375P cell line with IC50 values in sub-micromolar scale. In addition, compound 1d exerted high selectivity towards RAF1 serine/threonine kinase with 96.47% inhibition at 10 µ<span style="font-variant: small-caps;">M</span>, and IC50 of 0.96 µ<span style="font-variant: small-caps;">M</span>. This compound can possess antiproliferative activity against melanoma cells through inhibition of RAF1 kinase.
著者
-
Choi Jung
Department Of Agricultural Biotechnology Seoul National University
-
Choi Hong
College of Dentistry, Pusan National University
-
Oh Chang-Hyun
Center for Biomaterials, Korea Institute of Science and Technology
-
Cho Hye
Chemical Kinomics Research Center, Korea Institute of Science and Technology
-
El-Gamal Mohammed
Center for Biomaterials, Korea Institute of Science and Technology
-
Lee So
Chemical Kinomics Research Center, Korea Institute of Science and Technology
-
Sim Taebo
Chemical Kinomics Research Center, Korea Institute of Science and Technology
-
Kim Garam
College of Pharmacy, Chosun University
-
Yoo Kyung
Chemical Kinomics Research Center, Korea Institute of Science and Technology
関連論文
- 成犬ならびに老犬の歯状回と海馬におけるグリア線維酸性蛋白免疫染色性の変化(解剖学)
- 癲癇抵抗性及び感受性スナネズミの海馬における小膠細胞及び星状膠細胞マーカータンパク質の特異的免疫反応性(解剖学)
- 一過性大脳虚血を施したスナネズミ皮質体性感覚野におけるGlutamic acid decarboxylase 67免疫反応性ならびにタンパク質レベルの一過性増加(解剖学)
- 癪癇感受性スナネズミの視床下部室旁核におけるTyrosine hydroxylaseの減少(解剖学)
- スナネズミ十二指腸の筋層間神経叢におけるカルビンジンD-28k陽性ニューロンの年齢に伴う変化(解剖学)
- Gliosis in the Amygdala Following Myocardial Infarction in the Rat
- スナネズミ海馬CA1領域におけるイオン化カルシウム結合アダプター分子1の免疫反応性及びタンパクレベルの年齢に伴う変化(解剖学)
- 種々月齢の特発性高血圧ラット歯状回におけるDoublecortin陽性神経前駆細胞 : SDラットとの比較について(解剖学)
- 成犬と老犬の海馬CA1領域における脂質過酸化反応とCu,Zn-superoxide dismutaseの違い(解剖学)
- Anti-diabetic Activity of SMK001, a Poly Herbal Formula in Streptozotocin Induced Diabetic Rats : Therapeutic Study(Pharmacology)
- Fluorescent Calix[4]arene-appended Silica Nanotubes as Selective Chemosensor and Adsorbent for Pb^ Ion
- Antimutagenicity and Cytotoxicity of the Constituents from the Aerial Parts of Rumex acetosa(Pharmacognosy)
- ラット主嗅球におけるカルレチニン陽性傍糸球体細胞(Periglomerular cells)の生後変化(解剖学)
- Comparison of Density and Morphology of Neuroblasts in the Dentate Gyrus among Variously Aged Dogs, German Shepherds(Anatomy)
- Reduction of Calbindin D-28k-Immunoreactive Neurons in the Dog Dentate Gyrus
- Mineralocorticoid and glucocorticoid receptor expressions in astrocytes and microglia in the gerbil hippocampal CA1 region after ischemic insult
- Species-Difference of Cyclooxygenase-2 in the Hippocampus of Rodents
- Immunohistochemical Changes in Orexigenic and Anorexigenic Neuropeptides in the Rat Hypothalamus after Capsaicin Administration
- Ribosomal Protein S3 Immunoreactivity in the Young, Adult and Aged Gerbil Hippocampus
- Mucinous Eccrine Nevus
- Acute Generalized Exanthematous Pustulosis in a Six-Year-Old Boy
- Case of congenital esophageal stricture by ganglioneuroma and acro-flexural hyperpigmentation : A coincidence?
- Induction of ErbB2 by ultraviolet A irradiation : Potential role in malignant transformation of keratinocytes
- Neuronal Degeneration and Microglial Activation in the Ischemic Dentate Gyrus of the Gerbil
- Risk factors for the different types of chronic lung diseases of prematurity according to the preceding respiratory distress syndrome
- Clinical characteristics of chronic lung disease without preceding respiratory distress syndrome in preterm infants
- IS-74 A clinical study of depression symptoms during pregnancy(Group9 Perinatology2,International Session)
- Cytopathology of Cervical Cancer in Korea
- Recovery from tanning induced by narrow-band UVB phototherapy in brown-skinned individuals with psoriasis : Twelve-month follow-up
- Calcinosis cutis of the fingertip associated with Raynaud's phenomenon
- Eruptive pseudoangiomatosis
- Plasma Cell Cheilitis Treated with Intralesional Injection of Corticosteroids
- Clinical Utility of Pleural Fluid NT-pro Brain Natriuretic Peptide (NT-proBNP) in Patients with Pleural Effusions
- Correlation between Antioxidative Activities and Metabolite Changes during Cheonggukjang Fermentation
- A Correlation between Antioxidant Activity and Metabolite Release during the Blanching of Chrysanthemum coronarium L.
- GC-MS Based Metabolite Profiling of Rice Koji Fermentation by Various Fungi
- Significance of volcanogenic sediments in the Nogam Formation of the Pyeongan Group in Korea (South)
- Changes in Cyclooxygenase-2 Immunoreactivity in the Hippocampus in a Model of Streptozotocin-Induced Type 1 Diabetic Rats
- Metabolomics-Based Optimal Koji Fermentation for Tyrosinase Inhibition Supplemented with Astragalus Radix
- Flavusides A and B, Antibacterial Cerebrosides from the Marine-Derived Fungus Aspergillus flavus
- Possibility to Establish Chicken Stem Cell from Non-germline Tissue : Detection of Colony-forming Cells after Chicken Fibroblast Culture and Subsequent Stem Cell Characterization
- 癲癇抵抗性及び感受性スナネズミの海馬における小膠細胞及び星状膠細胞マーカータンパク質の特異的免疫反応性
- Real-Time Observation of Single-Electron Movement through Silicon Single-Electron Transistor
- Novel Quinolinylaminoisoquinoline Bioisosteres of Sorafenib as Selective RAF1 Kinase Inhibitors: Design, Synthesis, and Antiproliferative Activity against Melanoma Cell Line
- Inhibitory effects of a new 1H-pyrrolo[3,2-c]pyridine derivative, KIST101029, on activator protein-1 activity and neoplastic cell transformation induced by insulin-like growth factor-1
- Memory Effect in an Aluminum Single-Electron Floating-Node Memory Cell
- Diarylureas and Diarylamides with Pyrrolo[2,3-d]pyrimidine Scaffold as Broad-Spectrum Anticancer Agents
- Identification of a new phomoxanthone antibiotic from Phomopsis longicolla and its antimicrobial correlation with other metabolites during fermentation