Novel dihydroisoxazoline-alkyl carbon chain hybrid artemisinin analogues (artemalogs): synthesis and antitumor activities
Novel dihydroisoxazoline-alkyl carbon chain hybrid artemisinin analogues (artemalogs): synthesis and antitumor activities
复制标题
新型二氢异恶唑啉-烷基碳链杂化青蒿素类似物（artemalogs）：合成和抗肿瘤活性
DOI：
10.1039/c6ra17323c
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发表时间：
2016-01-01
期刊：
影响因子：
3.9
通讯作者：
Ding, Chunyong
中科院分区：
文献类型：
--
作者：
Liu, Gang;Song, Shanshan;Ding, Chunyong
通过1，3-偶极环加成反应设计并合成了两个新的二氢异恶唑啉-烷基碳链杂合青蒿素类似物（artemalogs）。随后的药理学筛选导致几种化合物与青蒿素和双氢青蒿素相比对几种人肿瘤细胞系具有显著改善的抗增殖作用。对最有效的蒿甲醚进行了机理研究。
Two new series of dihydroisoxazoline-alkyl carbon chain hybrid artemisinin analogues (artemalogs) were designed and synthesized though a 1,3-dipolar cycloaddition. Subsequent pharmacological screening led to several compounds having dramatically improved antiproliferative effects against several human tumor cell lines compared to artemisinin and dihydroartemisinin. Mechanistic studies on the most potent artemalogs were investigated.