20197-55-1

Upstream product

• 20332-16-5 4,5-methylenedioxyanthranilic acid 
• 40680-63-5 methyl 6-aminobenzo[d][1,3]dioxole-5-carboxylate 
• 721-00-6 methyl 6-nitrobenzo[d][1,3]dioxole-5-carboxylate 
• 326-56-7 methyl 3,4-methylenedioxybenzoate 
• 187164-87-0 5-amino-6-cyanobenzo<1,3>dioxale 
• 52805-38-6 6-nitro-1,3-benzodioxole-5-carbonitrile 
• 4421-09-4 piperonylonitrile 
• 53216-40-3 6-aminobenzo[d][1,3]dioxole-5-carboxamide 
• 66117-81-5 6-nitrobenzo[d][1,3]dioxole-5-carboxamide 
• 716-32-5 6-nitrobenzo[d][1,3]dioxole-5-carboxylic acid 
• 50425-29-1 4,5-methylenedioxy-2-nitrobenzoyl chloride 
• 94-53-1 Piperonylic acid 

Downstream Products

• 1458639-52-5 C₂₁H₂₁ClN₄O₂ 
• 1458639-32-1 C₂₆H₃₂N₆O₂ 
• 1458639-33-2 C₂₆H₃₁N₅O₂ 
• 1458639-34-3 C₃₀H₃₃N₇O₂ 

Relevant academic research and scientific papers

As the PI3K/mTOR inhibitor tricyclic compound, its preparation and use

The invention discloses a tricyclic compound as a PI3K/mTOR inhibitor. The tricyclic compound is a compound with the general formula (I) in the specification, wherein Ar is selected from aryl or heteroaryl; X, Y and Z are independently selected from O, CR2R3 and NR4 respectively; Q is selected from O, CR2R3 and NR4 or does not exists; R1 represents C1-C6 alkyl; n is selected from integers from 0 to 4; when n is more than or equal to 2, two R1 and a morpholine cycle can be combined into a combined cycle, a bridge cycle or a spiral cycle; R2 and R3 are selected from hydrogen and C1-C6 alkyl; R4 is selected from hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, heterocyclic radical, acyl and sulfonyl. The invention further discloses a perpetration method of the compound with the general formula (I) as well as a pharmaceutical composition and application of the compound with the general formula (I).

Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors

G9a is a histone lysine methyltransferase (HKMT) involved in epigenetic regulation via the installation of histone methylation marks. 6,7-Dimethoxyquinazoline analogues, such as BIX-01294, are established as potent, substrate competitive inhibitors of G9a. With an objective to identify novel chemotypes for substrate competitive inhibitors of G9a, we have designed and synthesised a range of heterocyclic scaffolds, and investigated their ability to inhibit G9a. These studies have led to improved understanding of the key pharmacophoric features of BIX-01294 and the identification of a new core quinoline inhibitory scaffold, which retains excellent potency and high selectivity. Molecular docking was carried out to explain the observed in vitro data. This journal is

Novel 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors

Novel 2-chloro-4-anilino-quinazolines designed as EGFR and VEGFR-2 dual inhibitors were synthesized and evaluated for inhibitory effects. EGFR and VEGFR-2 are validated targets in cancer therapy and combined inhibition might be synergistic for both antitumor activity and resistance prevention. The biological data obtained proved the potential of 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors, highlighting compound 8o, which was approximately 7-fold more potent on VEGFR-2 and approximately 11-fold more potent on EGFR compared to the prototype 7. SAR and docking studies allowed the identification of pharmacophoric groups for both kinases and demonstrated the importance of a hydrogen bond donor at the para position of the aniline moiety for interaction with conserved Glu and Asp amino acids in EGFR and VEGFR-2 binding sites.