Synthesis, cytotoxicities and DNA-binding affinities of benzofuran-3-ols and their fused analogs.
Synthesis, cytotoxicities and DNA-binding affinities of benzofuran-3-ols and their fused analogs.
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苯并呋喃-3-醇及其融合类似物的合成、细胞毒性和 DNA 结合亲和力。
DOI：
10.1248/cpb.59.1057
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发表时间：
2011
影响因子：
1.7
通讯作者：
Shu
中科院分区：
文献类型：
--
作者：
Zhong;Min Zou;Jia Zhou;Chun;Yan‐Hong Deng;Ming;Chun;Zhihong Jiang;Wen;Shu
由2-芳酰基苯并呋喃-3-醇1a-i与水合肼反应，合成了一系列苯并呋喃并吡唑类化合物2a-i，收率为10-92%，并筛选了它们对四种人实体瘤细胞系的抗肿瘤活性，包括胃癌细胞MKN 45、肝细胞癌细胞HepG 2、乳腺癌细胞MCF-7和肺癌细胞A549。结果表明，化合物1a-i和2a-i均具有一定的抗肿瘤活性。其中，化合物2 e对所有四种肿瘤细胞系均表现出有效的抑制活性。此外，化合物1 e和2 e显示出很强的DNA结合亲和力，并诱导小牛胸腺DNA的粘度增加，表明它们可能作为嵌入剂。
A series of benzofuropyrazoles 2a-i were synthesized in 10-92% from the reaction of 2-aroylbenzofuran-3-ols 1a-i with hydrazine hydrate, and screened for their antitumor activities toward four human solid tumor cell lines, including gastric carcinoma cells MKN45, hepatocellular carcinoma cells HepG2, breast cancer cells MCF-7, and lung cancer cells A549. The results indicated that both compounds 1a-i and 2a-i displayed moderate antitumor activities. Among them, compound 2e exhibited potent inhibitory activity toward all the four tumor cell lines. In addition, compounds 1e and 2e showed strong DNA-binding affinities, and induced an increase in the viscosity of calf-thymus DNA, suggesting that they might act as an intercalator.
影响因子：
2.8
作者：
Kim, Soyoung;Salim, Angela A.;Kinghorn, A. Douglas
通讯作者：
Kinghorn, A. Douglas