86671-87-6

Upstream product

• 106-47-8 4-chloro-aniline 
• 91-20-3 naphthalene 
• 1073-69-4 N-4-chlorophenylhydrazine 
• 528-46-1 phthalonic acid 
• 97458-95-2 methyl 4-oxo-3-(4-chlorophenyl)-3,4-dihydrophthalazine-1-carboxylate 
• 791638-32-9 2-[Methoxy(oxo)acetyl]benzoesaeure 
• 14736-50-6 o-(methoxycarbonylmethyl)benzoic acid 
• 703-59-3 homophthalic anhydride 
• 86671-86-5 4-(4-Chlorophenylhydrazono)-1H-2-benzopyran-1,3(4H)-dione 
• 86662-15-9 3-(4-chlorophenyl)-4-oxo-3,4-dihydrophthalazine-1-carboxylic acid 

Downstream Products

• 97458-97-4 2-(4-chlorophenyl)-4-hydroxymethyl-1(2H)-phthalazinone 
• 86690-22-4 3-(4-Chloro-phenyl)-4-oxo-3,4-dihydro-phthalazine-1-carboxylic acid (3-chloro-phenyl)-amide 
• 86671-84-3 3-(4-Chloro-phenyl)-4-oxo-3,4-dihydro-phthalazine-1-carboxylic acid (2-chloro-phenyl)-amide 
• 1415647-89-0 3-(4-chlorophenyl)-4-oxo-3,4-dihydrophthalazine-1-carbonyl azide 
• 1415647-96-9 methyl [3-(4-chlorophenyl)-4-oxo-3,4-dihydrophthalazin-1-yl]carbamate 
• 1415648-01-9 4-amino-2-(4-chlorophenyl)phthalazin-1(2H)-one 
• 86671-81-0 3-(4-Chloro-phenyl)-4-oxo-3,4-dihydro-phthalazine-1-carboxylic acid o-tolylamide 
• 86671-82-1 3-(4-Chloro-phenyl)-4-oxo-3,4-dihydro-phthalazine-1-carboxylic acid m-tolylamide 
• 86671-80-9 3-(4-Chloro-phenyl)-4-oxo-3,4-dihydro-phthalazine-1-carboxylic acid phenylamide 
• 86671-85-4 3-(4-Chloro-phenyl)-4-oxo-3,4-dihydro-phthalazine-1-carboxylic acid (4-chloro-phenyl)-amide 
• 86671-83-2 2-(4-Chlorophenyl)-4-(4-methylphenylaminocarbonyl)-1(2H)-phthalazinone 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of N-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-4-oxo-3,4-dihydrophthalazine-1-carboxamide derivatives as novel P-glycoprotein inhibitors reversing multidrug resistance

The overexpression of P-glycoprotein plays an important role in the process of multidrug resistance (MDR). P-gp inhibitors are one of the effective strategies to reverse tumor MDR. Novel P-gp inhibitors with phthalazinone scaffolds were designed, synthesized and evaluated. Compound 26 was found to be the most promising for further study. Compound 26 possessed high potency (EC50 = 46.2 ± 3.5 nM) and low cytotoxicity.26 possessed high MDR reversal activity towards doxorubicin-resistant K56/A02 cells. Reversal fold (RF) value reach to 44.26. 26 also increased accumulation of doxorubicin (DOX or ADM) or other MDR-related anticancer drugs with different structures. In conclusion, compound 26 deserves more research for its good features as P-gp inhibitor.

Synthesis and biological evaluation of 4-(2-fluorophenoxy)-3,3′-bipyridine derivatives as potential c-met inhibitors

Six series of novel 4-(2-fluorophenoxy)-3,3′-bipyridine derivatives conjugated with aza-aryl formamide/amine scaffords were designed and synthesized through a structure-based molecular hybridization approach. The target compounds were evaluated for c-Met kinase inhibitory activities and cytotoxicity against four cancer cell lines (HT-29, A549, MKN-45 and MDA-MB-231) in vitro. Most compounds exhibited moderate to excellent potency, and the most promising candidate 26c (c-Met kinase IC50 = 8.2 nM) showed a 4.7-fold increase in cytotoxicity against c-Met-addicted MKN-45 cell line in vitro (IC50 = 3 nM), superior to that of Foretinib (IC50 = 23 nM). The preliminary structure-activity relationship indicated that a 1H-benzo [e] [1,3,4]thiadiazine-3-carboxamide-4,4-dioxide moiety as linker contributed to the antitumor potency.

Facile synthesis of novel 7-aminofuro- and 7-aminothieno[2,3-d]pyridazin- 4(5H)-one and 4-aminophthalazin-1(2H)-ones

We hereby report the synthesis of a novel class of compounds, 7-aminofuro- and 7-aminothieno[2,3-d]pyridazin-4(5H)-one and 4-aminophthalazin-1(2H)-ones starting from methyl 2-(2-methoxy-2-oxoethyl)furan- and thiophene-3-carboxylate and methyl 2-(2-methoxy