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Design, synthesis and antiproliferative activity of novel 5-nitropyrimidine-2,4-diamine derivatives bearing alkyl acetate moiety.

Abstract：

:In order to discover new anticancer drug leads, a series of novel alkylamino pyrimidine derivatives were designed and synthesized based on our previous work via a ring-opening strategy. Biological evaluation with four human cancer cell lines (MDA-MB-231, A549, HepG2, and MCF-7) showed that most of these compounds possessed moderate to potent antiproliferative activities. The most promising compound 7w displayed a three-fold improvement compared with commercial anticancer drug fluorouracil in inhibiting HepG2 cell proliferation with IC50 value of 10.37 μM. Moreover, flow-activated cell sorting analysis suggested that compound 7w mainly arrested HepG2 cells in G2/M stage. Hence, it could serve as a promising lead for the design of novel anticancer small-molecule drugs.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Zhao PL,Li YH,Yang HK,Chen P,Zhang B,Sun Q,Li Q,You WW

doi

10.1016/j.ejmech.2016.04.038

subject

Has Abstract

pub_date

2016-08-08 00:00:00

pages

161-9

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30331-2

journal_volume

118

pub_type

杂志文章

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