284462-87-9

Upstream product

• 882167-77-3 4-chloro-N-methyl-pyridine-2-carboxamide hydrochloride 
• 1193-02-8 4-aminotiophenol 
• 24484-93-3 4-Chloro-pyridine-2-carboxylic acid methyl ester 
• 53750-66-6 4-chloro-pyridine-2-carbonyl chloride 
• 98-98-6 2-Picolinic acid 
• 220000-87-3 4-chloro-N-methylpicolinamide 

Downstream Products

• 1071534-78-5 4-(4-(4-(4-chlorophenyl)phthalazin-1-ylamino)phenylthio)-N-methylpicolinamide 
• 1393482-50-2 4-(4-(2,2-dichloroacetamido)phenylthio)-N-methylpicolinamide 
• 1393482-54-6 N-methyl-4-(4-propionamidophenylthio)picolinamide 
• 1313174-90-1 N-methyl-4-(4-pivalamidophenylthio)picolinamide 
• 1393482-43-3 4-(4-(2-chlorobenzamido)phenylthio)-N-methylpicolinamide 
• 1291103-20-2 4-(4-(3-methoxybenzamido)phenylthio)-N-methylpicolinamide 
• 1291103-22-4 N-methyl-4-(4-(3-(trifluoromethyl)benzamido)phenylthio)picolinamide 
• 1291103-25-7 N-methyl-4-(4-(4-(trifluoromethyl)benzamido)phenylthio)picolinamide 
• 1393482-40-0 4-(4-benzamidophenylthio)-N-methylpicolinamide 
• 1393482-41-1 4-(4-(4-methoxybenzamido)phenylthio)-N-methylpicolinamide 
• 1393482-49-9 N-methyl-4-(4-(4-nitrobenzamido)phenylthio)picolinamide 
• 1291103-21-3 4-(4-(3,5-dimethoxybenzamido)phenylthio)-N-methylpicolinamide 
• 1017375-26-6 4-(4-acetamidophenylthio)-N-methylpicolinamide 
• 1393482-55-7 4-(4-butyramidophenylthio)-N-methylpicolinamide 

Relevant academic research and scientific papers

Thiourea and thioether derivatives of sorafenib: Synthesis, crystal structure, and antiproliferative activity

A series of novel sorafenib derivatives containing diaryl thiourea and thioether, 9a-u, was designed and synthesized, and their antiproliferative activities against HCT116 and MDA-MB-231 cell lines were also evaluated and described. Most compounds exhibited potent antiproliferative activity against HCT116 cells with IC50 = 1.8-80.4 μM. Compounds 9p, 9r, and 9s demonstrated competitive antiproliferative activities to sorafenib, against all two cancer cell lines. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR, and HRMS, and compound 9n was characterized by single-crystal X-ray diffraction. Primary structure-activity relationships (SAR) have also been established.

ANTICANCER COMPOUNDS AND PREPARATION METHODS THEREOF

Two new compounds with anticancer effects of N-[4-chloro-3-(trifluoromethyl)phenyl]-[4-(N-methyl-formamide)(4-pyridyloxy)phenyl]-thiourea and N-[4-chloro-3-(trifluoromethyl)phenyl]-[4-(N-methyl-formamide)(4-pyridylthio)phenyl]-thiourea, and salts thereof are disclosed. Preparation methods of the two new compounds and pharmaceutical compositions containing the new compounds are further disclosed. Experimental studies show that the two new compounds can effectively inhibit the activity of Raf and VEGFR protein kinase, widely inhibit growth of various types of human tumor cell lines and further induce apoptosis of tumor cells. Human tumor heterograft model investigation proves that the two new compounds are effective antineoplastic agents, and can sharply inhibit growth of human liver cancer cells, lung cancer cells and intestinal cancer cells in vivo. Furthermore, the anticancer effects of the compounds are much better than that of Sorafenib.

Synthesis and biological evaluation of novel N-methyl-picolinamide-4-thiol derivatives as potential antitumor agents

A novel series of N-methylpicolinamide-4-thiol derivatives were synthesized and evaluated on human cancer cell lines. Among them, compound 6p displayed potent and broad-spectrum anti-proliferative activities in vitro on some human cancer cell lines, even better than sorafenib. The advanced kinase inhibitory assays showed that compound 6p could selectively inhibit Aurora-B kinase. The biological results were rationalized by the molecular docking study, which indicated the stable interactions of 6p with the Aurora-B kinase.

AURORA KINASE MODULATORS AND METHODS OF USE

The present invention relates to chemical compounds having a general formula I (I) wherein A1-6, L1, R1, R4-6 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinase proteins. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds and methods of treating disease states related to the activity of Aurora kinase.