Мақола

Design, synthesis, and toward a side-ring optimization of tricyclic thieno[2,3-<i>d</i>]pyrimidin-4(3<i>H</i>)-ones and their effect on melanin synthesis in murine B16 cells

Li Fei NieKey Laboratory of Plant Resources and Chemistry in Arid Regions, State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, P. R. China;Khurshed BozorovInstitute of the Chemistry of Plant Substances, Academy of Sciences of Uzbekistan, Tashkent, UzbekistanGuozheng HuangKey Laboratory of Plant Resources and Chemistry in Arid Regions, State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, P. R. China;Jiangyu ZhaoKey Laboratory of Plant Resources and Chemistry in Arid Regions, State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, P. R. China;Chao NiuKey Laboratory of Plant Resources and Chemistry in Arid Regions, State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, P. R. China;Haji Akber AisaKey Laboratory of Plant Resources and Chemistry in Arid Regions, State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, P. R. China;

Phosphorus, sulfur, and silicon and the related elementsjournal2018en

ABI

Аннотация

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.

Мавзулар

Quinazolinone synthesis and applications Phenothiazines and Benzothiazines Synthesis and Activities Synthesis and Characterization of Heterocyclic Compounds

Идентификаторлар

DOI: 10.1080/10426507.2018.1487968

Иқтибослар ва манбалар

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