Liu, Wenjing published the artcileDesign, synthesis and biological evaluation of novel 4-(4-methoxynaphthalen-1-yl)-5-arylpyrimidin-2-amines as tubulin polymerization inhibitors, SDS of cas: 104-01-8, the main research area is methoxynaphthalenylarylpyrimidinamine preparation tubulin polymerization inhibitor antitumor; anticancer; naphthalene; pyrimidine; tubulin polymerization inhibitor.
A novel series of 4-(4-methoxynaphthalen-1-yl)-5-arylpyrimidin-2-amines I (R = 4-OEt, 4-Me, 4-Cl, etc.) were designed, synthesized, and evaluated for their anticancer activities. Most of the synthesized compounds exhibited moderate to high antiproliferative activity in comparison to the standard drug cisplatin. Among them, I (R = 4-OEt) was found to be the most active on MCF-7 and HepG2 cancer cell lines, with IC50 values of 3.77 +/= 0.36 and 3.83 +/= 0.26μM, resp. Further mechanism study shown that I (R = 4-OEt) potently inhibited tubulin polymerization, induced cell cycle arrest at G2/M phase and cell apoptosis in MCF-7 cell line. Furthermore, mol. modeling study suggested that I (R = 4-OEt) probably binds to the colchicine site of tubulin.
Chemical & Pharmaceutical Bulletin published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, SDS of cas: 104-01-8.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem