482630-07-9

Upstream product

• 128071-75-0 2-bromopyridine-3-carboxaldehyde 
• 182163-96-8 3,4,5-trimethoxyphenylboronic Acid 
• 427886-33-7 3-hydroxymethyl-2-(3,4,5-trimethoxyphenyl)-pyridine 

Relevant academic research and scientific papers

Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin

Mimicking different pharmacophoric units into one scaffold is a promising structural modification tool to design new drugs with enhanced biological properties. To continue our research on the tubulin inhibitors, the synthesis and biological evaluation of arylpyridine derivatives (9-29) are described herein. Among these compounds, 6-arylpyridines (13-23) bearing benzo[d]imidazole side chains at the 2-position of pyridine ring displayed selective antiproliferative activities against HT-29 cells. More interestingly, 2-trimethoxyphenylpyridines 25, 27, and 29 bearing benzo[d]imidazole and benzo[d]oxazole side chains displayed more broad-spectrum antitumor activities against all tested cancer cell lines. 29 bearing a 6-methoxybenzo[d]oxazole group exhibited comparable activities against A549 and U251 cells to combretastatin A-4 (CA-4) and lower cytotoxicities than CA-4 and 5-Fu. Further investigations revealed 29 displays strong tubulin polymerization inhibitory activity (IC50 = 2.1 μM) and effectively binds at the colchicine binding site and arrests the cell cycle of A549 in the G2/M phase by disrupting the microtubules network.

Cyclic diamine compound with 6-membered ring groups

A cyclic diamine compound of formula (1): wherein A is a single bond or C≡C; X and Y are individually CH or a nitrogen atom; m is 1 or 2; and n is a number of 1 to 5; an acid-addition salt thereof, or a hydrate thereof. The compound has excellent inhibitory effects on both cell adhesion and cell infiltration and is useful as a medicine for prevention or treatment of diseases such as allergy, asthma, rheumatism, arteriosclerosis and inflammation.