Design, Synthesis, and Biological Evaluation of Artemisinin-Piperazine-Phosphoramide Mustard Hybrids as Potential Anticancer Agents,ChemMedChem

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Design, Synthesis, and Biological Evaluation of Artemisinin-Piperazine-Phosphoramide Mustard Hybrids as Potential Anticancer Agents
ChemMedChem ( IF 3.6 ) Pub Date : 2022-06-30 , DOI: 10.1002/cmdc.202200239
Meng-Xue Wei _{1,

2} , Si-Si Zhang ₁ , Xuanrong Sun ₃ , Yang Ji ₁ , Pei-Wen Yang ₁ , Xue-Qiang Li ₁

Affiliation

Twelve novel artemisinin-piperazine-phosphoramide mustard (PPM) hybrids 7 a–l were synthesized via an efficient, catalyst-free two-step sequential substitution. Artemisinin-PPM hybrids 7 showed better cytotoxicity than DHA and VCR. Cytotoxicity was significantly enhanced by the introduction of a thiazole moiety. Hybrid 7 h displayed 7.4-fold stronger potency than VCR, and is both the most potent compound synthesised, and the most selective (selectivity index=16).

中文翻译：

青蒿素-哌嗪-磷酰胺芥菜杂化物作为潜在抗癌剂的设计、合成和生物学评价

通过高效、无催化剂的两步顺序置换合成了12 种新型青蒿素-哌嗪-磷酰胺芥 (PPM) 杂化物7a - l 。Artemisinin-PPM 杂交体7表现出比 DHA 和 VCR 更好的细胞毒性。通过引入噻唑部分显着增强了细胞毒性。Hybrid 7 h显示出比 VCR 强 7.4 倍的效力，并且是合成的最有效的化合物，也是最具选择性的（选择性指数 = 16）。

更新日期：2022-06-30

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