34127-27-0

Upstream product

• 31143-83-6 ethyl 4-oxo-1,4-dihydro-2H-3,1-benzoxazine-2-carboxylate 
• 617-36-7 Ethyl oxamate 
• 1904-58-1 anthranilic acid hydrazide 
• 95-92-1 oxalic acid diethyl ester 
• 134-20-3 2-carbomethoxyaniline 
• 118-92-3 anthranilic acid 

Downstream Products

• 34127-29-2 3-phenyl-1H,3H-<1,2,4>triazino<6,1-b>quinazoline-2,4,10-trione 
• 140182-23-6 3-(4-Chloro-phenyl)-2-thioxo-2,3-dihydro-1H-1,3,9a,10-tetraaza-anthracene-4,9-dione 
• 140182-21-4 3-(4-Methoxy-phenyl)-2-thioxo-2,3-dihydro-1H-1,3,9a,10-tetraaza-anthracene-4,9-dione 

Relevant academic research and scientific papers

Pyridazino[1,6-b]quinazolinones as new anticancer scaffold: Synthesis, DNA intercalation, topoisomerase I inhibition and antitumor evaluation in vitro and in vivo

A new anticancer N-containing heterocyclic scaffold was designed and 30 pyridazino[1,6-b]quinazolinone derivatives were synthesized and characterized. Antiproliferation evaluation in vitro against four human cancer cell lines including SK-OV-3(ovarian cell), CNE-2(nasopharyngeal cell), MGC-803(gastric cell) and NCI-H460(lung cell) indicated that most of them exhibited potent anticancer activity and the IC50 value of the most potent compound lowered to sub-μM. DNA interaction assay indicated that compounds 4e, 4g, 6o, 6p, 8o can intercalate into DNA. Compounds 6 and 8 also demonstrated potent topoisomerase I (topo I) activity. Annexin V- FITC/propidium iodide dual staining assay and cell cycle analysis indicated that 2-(4-bromophenyl)-4-((3-(diethylamino)propyl)amino) ?10H-pyridazino [1,6-b]quinazolin- 10-one (8p) could induce arrest cell cycle at G2 phase and apoptosis in MGC-803 cells in a dose-dependent manner. The in vivo antitumor efficiency of compound 8p was also evaluated on MGC-803 xenograft nude mice, and the relative tumor growth inhibition was up to 55.9% at a dose of 20 mg/kg per two days. The results suggested that pyridazino[1,6-b]-quinazolinones might serve as a promising novel scaffold for the development of new antitumor agents.

Pyridazine [6, 1-b] and quinazolinone derivative, preparation method thereof and application of derivative

The invention provides a pyridazine [6, 1-b] and quinazolinone derivative, a preparation method thereof and an application of the derivative, and further particularly relates to a drug composition composing the compound and an application of the medicine composition to preparation of an anti-tumor drug. The compound is synthesized and reported for the first time and shows good anti-tumor activityin vitro.

Reactions of ethyl oxamate and dialkyl oxalates with anthranilic acid derivatives

Ethyl oxamate reacted with anthranilic acid derivatives at the amide or the ester group leading to the formation of respective esters or amides. A simple method was developed for preparation of alkyl 3-amino-4-oxo-3,4- dihydroquinazoline-2-carboxylates. Nauka/Interperiodica 2007.