Wang, Guangcheng published the artcileDesign, synthesis and biological evaluation of isoxazole-naphthalene derivatives as anti-tubulin agents, Quality Control of 104-01-8, the main research area is isoxazole naphthalenyl preparation antitumor activity mol docking.
In this study, a novel series of isoxazole-naphthalene hybrids I [R = 2-ClC6H4, 4-EtOC6H4, 3,4,5-(MeO)3C6H2, 2H-1,3-benzodioxol-5-yl, etc.] as tubulin polymerization inhibitors were designed, synthesized and evaluated for their anti-proliferative activities against human breast cancer cell line MCF-7. Most of the synthesized compounds I exhibited moderate to potent antiproliferative activity (IC50 < 10.0μM), as compared to cisplatin (15.24 ± 1.27μM). Among them, compound I (R = 4-EtOC6H4) was found to be the most active compound with IC50 value of 1.23 ± 0.16μM. Mechanistic studies revealed that this compound arrested cell cycle at G2/M phase and induced apoptosis. Furthermore, in vitro tubulin polymerization assay showed that the compound I (R = 4-EtOC6H4) displayed better inhibition activity on tubulin polymerization (IC50 = 3.4μM) than colchicine (IC50 = 7.5μM). Mol. docking study also revealed that this compound binds to the colchicine binding site of tubulin. Arabian Journal of Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Quality Control of 104-01-8.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem