5533-90-4

Upstream product

• 29668-44-8 2,3-dihydro-benzo[1,4]dioxin-6-carbaldehyde 
• 98-86-2 acetophenone 
• 139-85-5 3,4-dihydroxybenzaldehyde 

Downstream Products

• 1350927-71-7 5-(2,3-dihydro-1,4-benzodioxane-6-yl)-3-phenyl-4,5-dihydro-1H-pyrazole 
• 1422156-12-4 C₁₉H₁₈N₂O₃ 
• 93637-93-5 3-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-1-phenyl-propylamine 
• 93637-99-1 6-(3-Hydroxy-3-phenylpropyl)benzo-1,4-dioxane 
• 93637-88-8 3-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-1-phenyl-propan-1-one 

Relevant academic research and scientific papers

Dihydropyrazole derivatives containing benzo oxygen heterocycle and sulfonamide moieties selectively and potently inhibit COX-2: Design, synthesis, and anti-colon cancer activity evaluation

Cyclooxygenase-2 (COX-2) as a rate-limiting metabolism enzyme of arachidonic acid has been found to be implicated in tumor occurrence, angiogenesis, metastasis as well as apoptosis inhibition, regarded as an attractive therapeutic target for cancer therapy. In our research, a series of dihydropyrazole derivatives containing benzo oxygen heterocycle and sulfonamide moieties were designed as highly potent and selective COX-2 inhibitors by computer-aided drug analysis of known COX-2 inhibitors. A total of 26 compounds were synthesized and evaluated COX-2 inhibition and pharmacological efficiency both in vitro and in vivo with multi-angle of view. Among them, compound 4b exhibited most excellent anti-proliferation activities against SW620 cells with IC50 of 0.86 ± 0.02 μM than Celecoxib (IC50 = 1.29 ± 0.04 μM). The results favored our rational design intention and provides compound 4b as an effective COX-2 inhibitor available for the development of colon tumor therapeutics.

Preparation method of novel triaryl pyrazoline derivative, and applications of novel triaryl pyrazoline derivative in anticancer drugs

The invention discloses a preparation method of a novel triaryl pyrazoline derivative, and applications of the novel triaryl pyrazoline derivative, and belongs to the field of pharmaceutical chemistry. The novel triaryl pyrazoline derivative possesses hig

4,5-Dihydropyrazole derivatives containing oxygen-bearing heterocycles as potential telomerase inhibitors with anticancer activity

Telomere and telomerase were closely related to the occurrence and development of some cancers. After the key active site of telomerase was identified, to enhance the ability of dihydropyrazole derivatives to inhibit telomerase, we designed a series of novel 4,5-dihydropyrazole derivatives containing heterocyclic oxygen moiety based on previous studies. The telomerase inhibition assay showed that compound 10a displayed the most potent inhibitory activity with an IC50 value of 0.6 μM for telomerase. The antiproliferative assay showed that 10a exhibited high activity against human gastric cancer cell SGC-7901 with an IC50 value of 10.95 ± 0.60 μM. Flow cytometric analysis and western blot results showed that 10a induced both apoptosis and autophagy. A docking simulation showed that 10a could bind well to the active site of telomerase and act as a telomerase inhibitor. The 3D-QSAR model was also built to provide a more pharmacological understanding that could be used to design new agents with more potent telomerase inhibitory activity.

Synthesis, biological evaluation, 3D-QSAR studies of novel aryl-2H-pyrazole derivatives as telomerase inhibitors

A series of novel aryl-2H-pyrazole derivatives bearing 1,4-benzodioxan or 1,3-benzodioxole moiety were designed as potential telomerase inhibitors to enhance the ability of aryl-2H-pyrazole derivatives to inhibit telomerase, a target of anticancer. The telomerase inhibition tests showed that compound 16A displayed the most potent inhibitory activity with IC50 value of 0.9 μM for telomerase. The antiproliferative tests showed that compound 16A exhibited high activity against human gastric cancer cell SGC-7901 and human melanoma cell B16-F10 with IC50 values of 18.07 and 5.34 μM, respectively. Docking simulation showed that compound 16A could bind well with the telomerase active site and act as telomerase inhibitor. 3D-QSAR model was also built to provide more pharmacophore understanding that could be used to design new agents with more potent telomerase inhibitory activity.

Synthesis and antihepatotoxic activity of 5-(2,3-dihydro-1,4-benzodioxane- 6-yl)-3-substituted-phenyl-4,5-dihydro-1H-pyrazole derivatives

In continuance of our search for newer antihepatotoxic agents some novel pyrazoline derivatives containing 1,4-dioxane ring system were synthesized starting from 3-(2,3-dihydro-1,4-benzodioxane-6-yl)-1-substituted-phenylprop-2- en-1-one. Some of the synthesized compounds were evaluated for antihepatotoxic activity against CCl4-induced hepatotoxicity in rats. Among them some compounds have shown significant antihepatotoxic activity comparable to standard drug silymarin.