期刊
ACS OMEGA
卷 6, 期 40, 页码 26583-26600出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.1c03948
关键词
anticancer agents; antiproliferative activity; colchicine azide; colchicine triazole; click chemistry
In this study, a series of 1,4-disubstituted 1,2,3-triazoles were designed and synthesized, with compounds containing an ester or amide moiety in the fourth position of 1,2,3-triazole of 10-N-methylaminocolchicine showing the greatest therapeutic potential.
A series of 1,4-disubstituted 1,2,3-triazoles having 10-demethoxy-10-N-methylaminocolchicine core were designed and synthesized via the Cu(I)-catalyzed click reaction and screened for their in vitro cytotoxicity against four cancer cell lines (A549, MCF-7, LoVo, LoVo/DX) and one noncancerous cell line (BALB/3T3). Indexes of resistance (RI) and selectivity (SI) were also determined to assess the potential of the analogues to break drug resistance of the LoVo/DX cells and to verify their selectivity toward killing cancer cells over normal cells. The compounds with an ester or amide moiety in the fourth position of 1,2,3-triazole of 10-N-methylaminocolchicine turned out to have the greatest therapeutic potential (low IC50 values and favorable SI values), much better than that of unmodified colchicine or doxorubicin and cisplatin. Thus, they make a valuable clue for the further search for a drug having a colchicine scaffold.
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