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Biological activity of intervenolin analogs with a phenyl substituent.
The Journal of Antibiotics ( IF 3.3 ) Pub Date : 2017-Oct-11 , DOI: 10.1038/ja.2017.123
Hikaru Abe , Manabu Kawada , Masayuki Igarashi , Shun-ichi Ohba , Chigusa Hayashi , Chiharu Sakashita , Takumi Watanabe , Masakatsu Shibasaki

Intervenolin analogs with a phenyl substituent at the 2- or 3-position were synthesized. The compounds (3-11) showed weak or no inhibitory activity toward the growth of MKN-74 gastric adenocarcinoma cells, even in the presence or absence of the corresponding Hs738 stromal cells, whereas 2-substituted analogs exhibited selective anti-Helicobacter pylori activity. Introduction of a pendant side chain on the nitrogen alleviated their acute toxicity in mice. The 2-phenyl-substituted analogs are reasonable structural templates for structure-activity relationship studies toward the development of anti-H. pylori agents that do not affect human cells.The Journal of Antibiotics advance online publication, 11 October 2017; doi:10.1038/ja.2017.123.

中文翻译:

具有苯基取代基的间苯二酚类似物的生物活性。

合成了在2-或3-位具有苯基取代基的间苯二酚类似物。化合物(3-11)即使在存在或不存在相应的Hs738基质细胞的情况下,对MKN-74胃腺癌细胞的生长也显示出微弱或没有抑制活性,而2-取代的类似物表现出选择性的抗幽门螺杆菌活性。在氮上引入侧链侧链可减轻它们在小鼠中的急性毒性。2-苯基取代的类似物是用于抗-H发展的结构-活性关系研究的合理的结构模板。不影响人类细胞的幽门螺杆菌药物。《抗生素杂志》提前在线出版,2017年10月11日; doi:10.1038 / ja.2017.123。
更新日期:2017-10-11
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