49675-75-4

Upstream product

• 17420-30-3 5-nitroanthranilonitrile 
• 62-53-3 aniline 
• 39263-34-8 N′-(2-cyano-4-nitrophenyl)-N,N-dimethylformimidamide 
• 19815-16-8 4-chloro-6-nitro-quinazoline 

Relevant academic research and scientific papers

Large yellow acid anilinoquinazoline derivatives preparation and anti-tumor application

The invention discloses large yellow acid anilinoquinazoline derivatives preparation and for anti-tumor. In order to parietic acid as a lead compound, is introduced into the 4 - anilinoquinazoline structure, synthesis is contained and 1, 8 - [...] - 9, 10 - anthraquinone - N - (6 - amino - 4 - anilinoquinazoline) - 3 - carboxamides of the compound. Cell test Certificate, the class of compounds of the nasopharyngeal carcinoma cells, breast cancer cells, liver cancer cells and ovarian cancer cells with different degree suppression effect, can be used for anti-tumor pharmaceutical preparation.

4-Arylamino-6-nitroquinazolines: Synthesis and their activities against neglected disease leishmaniasis

4-Arylamino-6-nitroquinazolines (2-25) were synthesized and evaluated for their leishmanicidal activities against Leishmania major promastigotes in vitro with IC50 values Combining double low line 1.87-61.48 μM. Among the twenty four synthetic derivatives, 4-[4′-(methylsulfanyl)phenyl]amino-6-nitroquinazoline (21), and 4-(2′-methoxyphenyl)amino-6-nitroquinazoline (8) showed excellent antileishmanial activities with IC50 values 1.87 ± 0.31 and 4.37 ± 0.02 μM, respectively, more active than the standard drug, pentamidine (IC50 Combining double low line 5.09 ± 0.09 μM). Compound 16 (IC50 Combining double low line 6.53 ± 0.21 μM) displayed an activity comparable to the standard. Compounds 15 (IC50 Combining double low line 9.04 ± 0.03 μM), 18 (IC50 Combining double low line 12.28 ± 0.18 μM), 14 (IC50 Combining double low line 19.87 ± 0.22 μM), and 5 (IC50 Combining double low line 24.03 ± 2.71 μM) also showed good activities.

Microwave-accelerated Dimroth rearrangement for the synthesis of 4-anilino-6-nitroquinazolines. Application to an efficient synthesis of a microtubule destabilizing agent

A useful and rapid access to 4-anilino-6-nitroquinazolines was investigated in a multi-gram scale via microwave-accelerated condensation and Dimroth rearrangement of the starting anilines with imines obtained by reaction of anthranilonitriles with formamide dimethylacetal. A novel short and efficient route to Azixa (EPi28495, MPC-6827), a microtubule destabilizing agent and apoptosis inducer, was performed with success demonstrating that well controlled parameters offer comfortable using of microwave technology with safe and environmental benefits.

QUINAZOLINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF DIABETES AND OBESITY

The present invention relates to novel quinazoline derivatives effective in lowering blood glucose level and body weight, and a medicine for treatment and/or prevention of diabetes and/or obesity, which comprises the compound as an active ingredient.

Radiolabeled irreversible inhibitors of epidermal growth factor receptor tyrosine kinase and their use in radioimaging and radiotherapy

Radiolabeled epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors and their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as