91973-67-0

Upstream product

• 10400-19-8 3-pyridinecarbonyl chloride 
• 123-30-8 4-amino-phenol 
• 20260-53-1 pyridine-3-carbonyl chloride hydrochloride 
• 59-67-6 nicotinic acid 
• 626-55-1 3-Bromopyridine 
• 13939-06-5 molybdenum hexacarbonyl 
• 111359-74-1 4-[(tert-butyldimethylsilyl)oxy]aniline 

Downstream Products

• 548765-76-0 methyl-phenyl-carbamic acid 4-[(pyridine-3-carbonyl)-amino]-phenyl ester 
• 1454918-30-9 N-methyl-N-(4-(quinolin-2-ylmethyloxy)phenyl)nicotinamide 

Relevant academic research and scientific papers

Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors

Based on quinazoline, quinoxaline, and nitrobenzene scaffolds and on pharmacophoric features of VEGFR-2 inhibitors, 17 novel compounds were designed and synthesised. VEGFR-2 IC50 values ranged from 60.00 to 123.85 nM for the new derivatives compared to 54.00 nM for sorafenib. Compounds 15a, 15b, and 15d showed IC50 from 17.39 to 47.10 μM against human cancer cell lines; hepatocellular carcinoma (HepG2), prostate cancer (PC3), and breast cancer (MCF-7). Meanwhile, the first in terms of VEGFR-2 inhibition was compound 15d which came second with regard to antitumor assay with IC50 = 24.10, 40.90, and 33.40 μM against aforementioned cell lines, respectively. Furthermore, Compound 15d increased apoptosis rate of HepG2 from 1.20 to 12.46% as it significantly increased levels of Caspase-3, BAX, and P53 from 49.6274, 40.62, and 42.84 to 561.427, 395.04, and 415.027 pg/mL, respectively. Moreover, 15d showed IC50 of 253 and 381 nM against HER2 and FGFR, respectively.

A new series of aryl sulfamate derivatives: Design, synthesis, and biological evaluation

Steroid sulfatase (STS) has recently emerged as a drug target for management of hormone-dependent malignancies. In the present study, a new series of twenty-one aryl amido-linked sulfamate derivatives 1a-u was designed and synthesized, based upon a cycloh

Small molecule compounds, and application thereof in preparation of anti-tumor metastasis drugs

The invention belongs to the technical field of medicines, and particularly relates to small molecule compounds, and application thereof in preparation of anti-tumor metastasis drugs. The preparationmethod comprises the following steps: preparing an inter

Aminocarbonylation of N -Containing Heterocycles with Aromatic Amines Using Mo(CO) 6

We describe herein the palladium-catalyzed aminocarbonylation of nitrogen-containing heterocycles with aniline derivatives using molybdenum hexacarbonyl as a CO solid source, expanding the scope of the limited examples. This method is compatible with a variety of substitutions on the aniline moiety. The simple reaction conditions include easily available Pd(dppf)Cl 2 catalyst, DBU as base in DMF at 120 °C for 3 hours in sealed tube thereby leading to the isolation of 21 compounds with yields ranging from 18 to 82%. We also show that double aminocarbonylation reactions are possible in satisfactory yields regarding both coupling partners.

Structure–activity relationship investigation of benzamide and picolinamide derivatives containing dimethylamine side chain as acetylcholinesterase inhibitors

A series of benzamide and picolinamide derivatives containing dimethylamine side chain (4a–4c and 7a–7i) were synthesised and evaluated for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity in vitro. Structure–activity relat

POLAROGRAPHIC REDUCTION OF 1-BENZYL-N-(p-X-PHENYL)-3-AMINOCARBONYLPYRIDINIUM SALTS

The substitution effect of different groups X (N(CH2CH3)2, OH, OCH3, CH3, NHCOCH3, H, Cl, COOCH2CH3 and NO2) on the polarographic behaviour of 3-(N-p-X-phenylaminocarbonyl)pyridines (I),1-benzyl-N-(p-X-phenyl)-3-aminocarbonylpyridinium cations (II) and their respective 1,4-dihydroderivatives (III) has been investigated in anhydrous solution of dimethylformamide with 0.1 mol 1-1 (n-C4H9)4N+PF6- as supporting electrolyte.The half-wave potentials of the reduction wave of I and II, which correspond to the uptake of a single electron (wave B) and to the formation of a primary radical, obey a Hammett correlation in a similar way as it is in the case of 1-benzyl- and 1-phenyl-3-amino-carbonylopyridinium cations substituted at carbon 4 on the benzene nucleus.The slope q?,R in the Hammett plot equals 0.192 V (I) and 0.104 V (II) for anhydrous DMF and compares thus with this slope obtained with the 1-benzyl- and 1-phenyl derivatives in our previous communications.