期刊
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
卷 193, 期 10, 页码 656-667出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/10426507.2018.1487968
关键词
Thieno[2,3-d]pyrimidin-4(3H)-ones; sulfonylamides; ipso-nitration; melanin synthesis; murine B16 cells
资金
- Chinese Academy of Sciences President's International Fellowship Initiative [2016PT014]
- National Natural Science Foundation of China (NSFC) [21550110495]
Herein, we report the synthesis of 48 novel 3-sulfonylamides containing a tricyclic thieno[2,3-d]pyrimidin-4(3H)-one moiety, and their influence on melanin synthesis in murine B16 cells. All target sulfonylamides were synthesized through key intermediate 3-nitro-thieno[2,3-d]pyrimidin-4(3H)-ones using three types of ipso-nitration reactions. In this case, we converted the pyrido[1,2-a]- fragment of the thieno[2,3-d]pyrimidine moiety to pyrrolo[1,2-a]- and azepino[1,2-a]- side-rings in order to evaluate the bioactivities of the synthesized derivatives for a structure activity-relationships point of view. The obtained results suggest that some of the selected compounds revealed a promising influence on melanin synthesis in murine B16 cells and may serve as lead compounds for further drug discovery and development. [GRAPHICS] .
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