76809-60-4

Upstream product

• 16634-82-5 N-(p-tolyl)-2-chloroacetamide 
• 106-49-0 p-toluidine 

Downstream Products

• 76809-77-3 N-benzylidene-(4-methylphenyl)-carbamoylmethylamine N-oxide 
• 302542-57-0 2-pyrazol-1-yl-N-p-tolyl-acetamide 
• 302542-60-5 2-(3,5-dimethylpyrazol-1-yl)-4'-methylacetanilide 
• 302542-63-8 2-(4-iodo-3,5-dimethyl-pyrazol-1-yl)-N-p-tolyl-acetamide 
• 76809-97-7 2-hydroxyamino-N-(4-methylphenyl)acetamide 
• 76810-16-7 1-(4-methylphenyl)-2(1H)-pyrazinone 4-oxide 
• 1240510-35-3 N-(N-p-tolylcarbamoylmethyl)-6,7-dimethoxy-3,3-dimethyl-3,4-dihydroisoquinolinium iodide 
• 1385049-57-9 2-(3-acetamido-6-methoxy-2-oxo-2H-chromen-7-yloxy)-N-(p-tolyl)acetamide 
• 1386999-97-8 2-(6-methoxy-2-oxo-2H-chromen-7-yloxy)-N-p-tolylacetamide 
• 3085-54-9 N-(4-methylphenyl)formamide 

Relevant academic research and scientific papers

Synthesis and evaluation of moxifloxacin derivatives for effects on proliferation and apoptosis of NCI-H1299 cells

Eight novel moxifloxacin (MXF) derivatives 4a-h were synthesized by functional modification of the N-5-Aza ring. Their growth inhibitory activities on human non-small lung cancer cell NCI-H1299 and A549 were evaluated by the MTT colorimetric assay. Based on the half inhibitory concentration (IC50) values, we determined that compounds 4b was the most efficacious derivative (IC50 = 2.56 ± 0.07 μM for NCI-H1299 and IC50 = 13.69 ± 0.70 μM for A549, respectively) that inhibited the proliferation of NCI-H1299 cells. Of these, Compound 4b (1 – cyclopropyl – 6 – fluoro – 8 – methoxy – 4 – oxo – 7 – ((4aS,7aS) – 1 – (2 – oxo – 2 – (p – tolylamino) ethyl) hexahydro – 1H – pyrrolo [3,4-b] pyridine – 6(2H)-yl) – 1,4 – dihydroquinoline – 3-carboxylic acid) showed good potency against the growth of NCI-H1299 cells and also selectivity on HUVEC cells (IC50 > 500 μM). The dose-response relationship of the characteristic morphological changes of NCI-H1299 cells induced by Compound 4b was confirmed by AO/EB fluorescent staining. Furthermore, Compound 4b triggered apoptosis of NCI-H1299 in a concentration-dependent manner and arrested cells in the G0/G1 phase. These data indicate that the N-(p-tolyl)propanamide functionalized N-5-Aza ring of moxifloxacin may be a promising lead compound and candidate for the development of new agents against non-small-cell lung cancer.

Synthesis and in vitro antitumor activity of novel scopoletin derivatives

Twenty scopoletin derivatives were developed by a systematic combinatorial chemical approach and their chemical structures were confirmed by MS, IR, 1H NMR spectra and elemental analysis. Primary screening against mammary (MCF-7 and MDA-MB 231) and colon (HT-29) carcinoma cells indicated that five compounds (8d, 8g, 8j, 11b and 11g) displayed high antitumor potencies with IC50 values below 20 μM whereas scopoletin showed IC50 values above 100 μM. Moreover, the most promising compound 11g was more active than 5-fluorouracil. These results clearly indicated that the modification of the scopoletin structure could greatly increase its antitumor activity in vitro.

Synthesis and NMR study of 2-[N-(Aryl)carbamoylmethyl]phthalazimum iodides

2-[N-(Aryl)carbamoylmethyl]phthalazinium iodides 11b-k were obtained, for the first time, by reaction between N-aryl-2-iodoacetamides 9b-k and phthalazine (10). The parent compound 11a was prepared by quaternization of phthalazine with iodoacetamide. The structure of the quaternary salts 11a-k was investigated by NMR experiments, namely HH-COSY, 1H- 13C-COSY and NOE.