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Arteminolides B, C, and D, new inhibitors of farnesyl protein transferase from Artemisia argyi.
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2002-10-26 , DOI: 10.1021/jo020299z Seung-Ho Lee 1 , Hyae-Kyeong Kim , Jeong-Min Seo , Hyun-Mi Kang , Jong Han Kim , Kwang-Hee Son , Heesoon Lee , Byoung-Mog Kwon , Jongheon Shin , Youngwan Seo
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2002-10-26 , DOI: 10.1021/jo020299z Seung-Ho Lee 1 , Hyae-Kyeong Kim , Jeong-Min Seo , Hyun-Mi Kang , Jong Han Kim , Kwang-Hee Son , Heesoon Lee , Byoung-Mog Kwon , Jongheon Shin , Youngwan Seo
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Arteminolides B-D (2-4), new farnesyl protein transferase inhibitors, were isolated together with a known arteminolide A (1) and new regioisomers (5-7) of the compounds from the aerial parts of Artemisia argyi. Structures of these compounds were elucidated by spectroscopic methods and chemical conversion. Arteminolides inhibited the farnesyl protein transferase with IC(50) values of 0.7-1 microM, while the regioisomers 5-7 were inactive. In addition, it was proved that the exocyclic double bond of sesquiterpene lactone did not affect the inhibitory activity of arteminolide. The effects of compound 2 on H-Ras processing and cellular growth in H-ras-transformed cells were also evaluated.
中文翻译:
青蒿素B,C和D,一种来自银蒿的法呢基蛋白转移酶的新抑制剂。
从蒿蒿的地上部分分离了新的法呢基蛋白转移酶抑制剂青蒿内酯BD(2-4)和已知的青蒿内酯A(1)和新的区域异构体(5-7)。通过光谱方法和化学转化来阐明这些化合物的结构。青蒿内酯抑制法呢基蛋白转移酶,其IC(50)值为0.7-1 microM,而区域异构体5-7则无活性。此外,已证明倍半萜内酯的环外双键不影响青蒿内酯的抑制活性。还评估了化合物2对H-ras转化细胞中H-Ras加工和细胞生长的影响。
更新日期:2019-11-01
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
青蒿素B,C和D,一种来自银蒿的法呢基蛋白转移酶的新抑制剂。
从蒿蒿的地上部分分离了新的法呢基蛋白转移酶抑制剂青蒿内酯BD(2-4)和已知的青蒿内酯A(1)和新的区域异构体(5-7)。通过光谱方法和化学转化来阐明这些化合物的结构。青蒿内酯抑制法呢基蛋白转移酶,其IC(50)值为0.7-1 microM,而区域异构体5-7则无活性。此外,已证明倍半萜内酯的环外双键不影响青蒿内酯的抑制活性。还评估了化合物2对H-ras转化细胞中H-Ras加工和细胞生长的影响。