21333-02-8

Upstream product

• 873-83-6 4-Amino-2,6-dihydroxypyrimidine 
• 106-47-8 4-chloro-aniline 
• 4270-27-3 6-chlorouracil 
• 67-52-7 BARBITURIC ACID 

Downstream Products

• 90987-47-6 10-(4-chlorophenyl)-2H,3H,4H,10H-pyrimido[4,5-b] quinol-ine-2,4-dione 
• 1079130-25-8 C₃₈H₄₈ClN₃O₂ 
• 90987-48-7 8-chloro-10-(4-chlorophenyl)-2H,3H,4H,10H-pyrimido[4,5-b]quinoline-2,4-dione 

Relevant academic research and scientific papers

UV365 light promoted catalyst-free synthesis of pyrimido[4,5-b] quinoline-2,4-diones in aqueous-glycerol medium

Herein, a highly efficient and environmentally benign protocol for the synthesis of biologically important pyrimido[4,5-b]quinolinone-2,4-diones from aromatic amines, barbituric acid and aryl aldehyde is reported. This process takes place at room temperat

5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2

Based on previous reports of certain 5-deazaflavin derivatives being capable of activating the tumour suppressor p53 in cancer cells through inhibition of the p53-specific ubiquitin E3 ligase HDM2, we have conducted an structure-activity relationship (SAR) analysis through systematic modification of the 5-deazaflavin template. This analysis shows that HDM2-inhibitory activity depends on a combination of factors. The most active compounds (e.g., 15) contain a trifluoromethyl or chloro substituent at the deazaflavin C9 position and this activity depends to a large extent on the presence of at least one additional halogen or methyl substituent of the phenyl group at N10. Our SAR results, in combination with the HDM2 RING domain receptor recognition model we present, form the basis for the design of drug-like and potent activators of p53 for potential cancer therapy.

Synthesis, biological active molecular design, and molecular docking study of novel deazaflavin-cholestane hybrid compounds

Novel deazaflavin-cholestane hybrid compounds, 3′,8′-disubstituted-5′-deazacholest-2,4-dieno[2,3-g]pteridine-2′,4′(3′H,8′H)-diones, have been synthesized by condensation reaction between 6-(monosubstituted amino)-pyrimidin-2,4(1H,3H)-diones and 2-hydroxymethylenecholest-4-en-3-one in presence of p-toluenesulfonic acid monohydrate and diphenyl ether. The antitumor activities against human tumor cell lines (CCRF-HSB-2 and KB cells) have been investigated in vitro, and many of these compounds showed promising antitumor activities. Furthermore, molecular docking study using LigandFit within the software package Discovery Studio 1.7 was done for lead optimization of these compounds as potential PTK inhibitors. In general, all of the synthesized steroid-hybrid compounds showed good binding affinities into PTK (PDB code: 1t46).

Synthesis of 5-deazaflavin derivatives and their activation of p53 in cells

A family of 5-deazaflavin derivatives has been synthesised using a two-step convergent strategy. The biological activity of these compounds was evaluated in cells, by assessing their ability to stabilize and activate p53. These compounds may act as low molecular weight inhibitors of the E3 activity of HMD2 in tumours that retain wild-type p53. Importantly, we have demonstrated that the nitro group present in all three of the original lead compounds [1-3 (HL198C-E)] is not essential for observation of this biological activity.

Flavins as Potential Antimalarials. 1. 10-(Halophenyl)-3-methylflavins

A series of 10-(halomethyl)-3-methylflavins was prepared by the condensation of 6-(haloanilino)-3-methyluracils with nitrosobenzene.A number of these flavins effectively cured lethal Plasmodium vinckei malarial infections in mice when administered by eith