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Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents.
ACS Omega ( IF 3.7 ) Pub Date : 2019-12-27 , DOI: 10.1021/acsomega.9b02600 Lorenzo Botta 1 , Silvia Filippi 1 , Bruno M Bizzarri 1 , Claudio Zippilli 1 , Roberta Meschini 1 , Rebecca Pogni 2 , Maria Camilla Baratto 2 , Luciano Villanova 3 , Raffaele Saladino 1
ACS Omega ( IF 3.7 ) Pub Date : 2019-12-27 , DOI: 10.1021/acsomega.9b02600 Lorenzo Botta 1 , Silvia Filippi 1 , Bruno M Bizzarri 1 , Claudio Zippilli 1 , Roberta Meschini 1 , Rebecca Pogni 2 , Maria Camilla Baratto 2 , Luciano Villanova 3 , Raffaele Saladino 1
Affiliation
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A library of hybrid and dimer compounds based on the natural scaffold of artemisinin was synthesized. These derivatives were obtained by coupling of artemisinin derivatives, artesunate, and dihydroartemisinin with a panel of phytochemical compounds. The novel artemisinin-based hybrids and dimers were evaluated for their anticancer activity on a cervical cancer cell line (HeLa) and on three complementary metastatic melanoma cancer cell lines (SK-MEL3, SK-MEL24, and RPMI-7951). Two hybrid compounds obtained by coupling of artesunate with eugenol and tyrosol, and one of the dimer compounds containing curcumin, emerged as the most active and cancer-selective derivatives.
中文翻译：
以青蒿素为基础的杂交和二聚体衍生物作为抗炭疽病药物的合成和评价。
合成了基于青蒿素天然支架的杂合和二聚体化合物文库。这些衍生物是通过将青蒿素衍生物，青蒿琥酯和二氢青蒿素与一组植物化学化合物偶联而获得的。评价了基于青蒿素的新型杂种和二聚体对宫颈癌细胞系（HeLa）和三种互补的转移性黑色素瘤癌细胞系（SK-MEL3，SK-MEL24和RPMI-7951）的抗癌活性。青蒿琥酯与丁子香酚和酪醇偶联获得的两种杂合化合物，以及一种含有姜黄素的二聚体化合物，表现出最具活性和对癌症的选择性。
更新日期：2020-01-14
中文翻译：
以青蒿素为基础的杂交和二聚体衍生物作为抗炭疽病药物的合成和评价。
合成了基于青蒿素天然支架的杂合和二聚体化合物文库。这些衍生物是通过将青蒿素衍生物，青蒿琥酯和二氢青蒿素与一组植物化学化合物偶联而获得的。评价了基于青蒿素的新型杂种和二聚体对宫颈癌细胞系（HeLa）和三种互补的转移性黑色素瘤癌细胞系（SK-MEL3，SK-MEL24和RPMI-7951）的抗癌活性。青蒿琥酯与丁子香酚和酪醇偶联获得的两种杂合化合物，以及一种含有姜黄素的二聚体化合物，表现出最具活性和对癌症的选择性。
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