Synthesis, Crystal Structure and Biological Activity of 6-Arylmethyl-7H-thiazolo[3,2-b]-1,2,4-triazin-7-one Derivatives as Antitumor Agents

关键词：2 derivatives synthesis crystal structure 

摘要：In order to explore the novel anti-tumor agents,ten 6-arylmethyl-3-aryl-777-thiazolo[3,2-b],2,4-triazin-7-ones were designed and synthesized,and the structures were characterized by ^1H-NMR,MS,IR and X-ray single-crystal diffraction analysis.The biological activity results showed that the target compounds exhibited certain inhibitory activity of osteosarcoma cells U2OS-EGFP.Compounds 6a,6g and 6j exhibited more than 70%inhibition ratio at the concentration of 50μmol·L^-1,and especially,the IC5o value of compound 6j was 11.58μmol·L^-1.The crystal of 6h was obtained and analyzed;some related weak interactions were discussed.The molecular docking results showed that the target compounds were supposed to be ERK1/2 inhibitors.

结构化学杂志要求:

{1}引言：概述与本文立题相关的有关报道及当前存在的问题，重点说明本研究的理论依据、研究思路、实验基础及国内外现状，阐述本文的目的，简述立题调研、文献分析，以及查阅方法、结论等。

{2}请勿一稿多投，自投稿之日起1个月内未收到采用意见，作者可自行处理。

{3}稿件应有中文摘要、关键词、英文题目及内容提要。稿件格式请参照附件——书稿规范进行处理。

{4}来稿请注明作者真实姓名、通信地址及邮政编码、联系电话等，以便联系。

{5}基金项目：指文章产出的资金背景。如国家社会科学基金，教育部博士点基金等。获得基金项目的文章应注明其名称，并在圆括号内注明其项目编号。

注：因版权方要求，不能公开全文，如需全文，请咨询杂志社