5443-31-2

Usage

InChI:InChI=1/C10H11N3/c1-6-4-9(12)8-5-7(11)2-3-10(8)13-6/h2-5H,11H2,1H3,(H2,12,13)

Upstream product

• 100795-23-1 N-(4-methoxy-2-methyl-6-quinolyl)acetamide 
• 631-61-8 ammonium acetate 
• 63304-46-1 N-(4-amino-2-methyl-quinolin-6-yl)-acetamide 
• 50593-73-2 4-chloro-6-methoxy-2-methylquinoline 
• 15644-90-3 6-methoxy-2-methylquinolin-4-ol 
• 33240-23-2 ethyl 3-((4-methoxyphenyl)amino)but-2-enoate 
• 75896-60-5 4,6-dimethoxy-2-methylquinoline 
• 104-94-9 4-methoxy-aniline 
• 611-09-6 5-nitroisatin 
• 122-80-5 N-acetyl-p-phenylenediamine 
• 1140-81-4 N-(4-hydroxy-2-methylquinolin-6-yl)acetamide 
• 17420-30-3 5-nitroanthranilonitrile 
• 99185-71-4 4-amino-2-methyl-6-nitroquinoline 
• 657375-22-9 4-chloro-2-methyl-[6]quinolylamine 

Downstream Products

• 101895-82-3 phenyl-propiolic acid-(4-amino-2-methyl-[6]quinolylamide) 
• 3811-56-1 surfen 
• 109939-01-7 N-(2-ethoxy-phenyl)-N'-(4-amino-2-methyl-[6]quinolyl)-urea 
• 6955-00-6 N-(4-amino-2-methyl-[6]quinolyl)-lauramide 
• 7511-76-4 N-(4-amino-2-methyl-[6]quinolyl)-nonanamide 
• 130672-04-7 N-(4-amino-2-methyl-[6]quinolyl)-N'-(3-nitro-phenyl)-urea 
• 102029-13-0 4-formyl-benzoic acid-(4-amino-2-methyl-[6]quinolylamide) 
• 109691-56-7 4-chloro-trans-cinnamic acid-(4-amino-2-methyl-[6]quinolylamide) 
• 112552-03-1 N-(4-amino-2-methyl-[6]quinolyl)-N'-biphenyl-2-yl-urea 
• 6269-69-8 2,4-dichloro-trans-cinnamic acid-(4-amino-2-methyl-[6]quinolylamide) 
• 109559-26-4 N-(4-amino-2-methyl-[6]quinolyl)-N'-m-tolyl-urea 
• 102026-60-8 2-methyl-N⁶-(4-nitro-benzyl)-quinoline-4,6-diyldiamine 
• 109559-27-5 N-(4-amino-2-methyl-[6]quinolyl)-N'-(2-methoxy-phenyl)-urea 
• 112551-67-4 N-(4-amino-2-methyl-[6]quinolyl)-N'-biphenyl-4-yl-urea 

Relevant academic research and scientific papers

FLUORESCENT PROBES FOR DRUG PERMEABILITY IN GRAM NEGATIVE BACTERIA

Described are compounds and methods useful in measuring membrane permeability and efflux transporter activity in bacteria, including multidrug resistance Gram negative bacteria.

5 - Fluoro - 2, 4 - disubstituted amino pyrimidine derivative and its preparation and use

The invention belongs to the field of chemical medicine and particularly relates to a 5-fluorine-2,4-bis-substituted aminopyrimidine derivative and a preparation method and application thereof. The structure of the 5-fluorine-2,4-bis-substituted aminopyri

A method for inhibiting PRMT7 compound and its preparation method and application (by machine translation)

The invention belongs to the field of chemical medicine, and in particular relates to a method for inhibiting PRMT7 compound, its formula is as follows: In some embodiments of the compounds proved that, this compound can to PRMT7 produce better inhibitio

Design, synthesis and anti leukemia cells proliferation activities of pyrimidylaminoquinoline derivatives as DOT1L inhibitors

A series of novel pyrimidylaminoquinoline derivatives 8(a-i) and 9(a-i) containing amino side chain, and the bisaminoquinoline analogs 3(b-e) have been designed and synthesized by structural modifications on a lead DOT1L inhibitor, 3a. All the compounds have been evaluated for their DOT1L inhibitory activities. The results showed that most of the compounds have strong anti DOT1L activities. Compounds 3e, 8h and 9e are the most potential ones from each category with the IC50 values of 1.06 ± 0.35 μM, 5.72 ± 1.56 μM and 3.55 ± 1.28 μM, respectively. Such inhibitors expressed significant binding interactions with DOT1L by surface plasmon resonance (SPR)-based binding assay. The results of molecular docking experiments suggested that they could occupy the SAM binding pocket of DOT1L. Compounds 8h and 9e exhibited better inhibitory activities but poor selectivities against the both MLL-rearranged MV4-11 cells and the non MLL-rearranged Kasumi-1 cells than those of 3a and 3e, which suggested that the introduction of the amino side chain would be beneficial for their anti leukemia cells proliferation activities, possibly due to the improvement of the fat solubility. Additionally, the direct cellular inhibition activities were found that compound 9e could effectively down-regulate both the level of H3k79 methylation and MLL-rearranged leukemia gene expression of Hoxa9 and Meis1 in MV4-11 in the qRT-PCR and western blot studies. These observations suggested DOT1L was one of the potential targets but perhaps not the most pivotal one for these compounds, which made their poor selectivities against leukemia cells proliferation.

Small molecule antagonists of cell-surface heparan sulfate and heparin-protein interactions

Surfen, bis-2-methyl-4-amino-quinolyl-6-carbamide, was previously reported as a small molecule antagonist of heparan sulfate (HS), a key cell-surface glycosaminoglycan found on all mammalian cells. To generate structure-activity relationships, a series of rationally designed surfen analogs was synthesized, where its dimeric structure, exocyclic amines, and urea linker region were modified to probe the role of each moiety in recognizing HS. An in vitro assay monitoring inhibition of fibroblast growth factor 2 binding to wild-type CHO cells was utilized to quantify interactions with cell surface HS. The dimeric molecular structure of surfen and its aminoquinoline ring systems was essential for its interaction with HS, and certain dimeric analogs displayed higher inhibitory potency than surfen and were also shown to block downstream FGF signaling in mouse embryonic fibroblast cells. These molecules were also able to antagonize other HS-protein interactions including the binding of soluble RAGE to HS. Importantly, selected molecules were shown to neutralize heparin and other heparinoids, including the synthetic pentasaccharide fondaparinux, in a factor Xa chromogenic assay and in vivo in mice. These results suggest that small molecule antagonists of heparan sulfate and heparin can be of therapeutic potential for the treatment of disorders involving glycosaminoglycan-protein interactions.

Synthesis and antibacterial activities of some substituted quinolines

p-Anisidine (1) on treatment with ethyl acetoacetate in refluxing ethanol for 4 h gave ethyl-3-[(4-methoxyphenyl)imino]butanoate (2) which on thermal cyclization in hot Dowtherm oil at 250 °C gave 4-hydroxy-6-methoxy-2-methylquinoline (3). The latter on h

GTPase inhibitors and methods of use and crystal structure of RAC-1 GTPase

The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchan

4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists

Structure-activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated.

GTPASE INHIBITORS AND USE THEREOF FOR CONTROLLING PLATELET HYPERACTIVITY

The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchan

GTPASE INHIBITORS AND METHODS OF USE

The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchan