Abstract:
:This study reports the synthesis of a series of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes, which are potent antitubulin agents. Compound 13, (2-hydroxy-3,4,5-trimethoxyphenyl)-(6-methoxy-1H-indol-3-yl)-methanone exhibits marked antiproliferative activity against KB and MKN45 cells with IC50 values of 8.8 and 10.5 nM, respectively, binds strongly to the colchicine binding site and leads to inhibition of tubulin polymerization. It also behaves as a vascular disrupting agent which suppresses the formation of capillaries. The C2-OH group in the A-ring of this compound not only retains the biological activity but has valuable physicochemical properties.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Lee HY,Chang CY,Lai MJ,Chuang HY,Kuo CC,Chang CY,Chang JY,Liou JPdoi
10.1016/j.bmc.2015.06.043subject
Has Abstractpub_date
2015-08-01 00:00:00pages
4230-4236issue
15eissn
0968-0896issn
1464-3391pii
S0968-0896(15)00537-4journal_volume
23pub_type
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