Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
复制标题
DOI：
10.1021/jm801484v
复制
发表时间：
2009-02-26
影响因子：
7.3
通讯作者：
Posner GH
中科院分区：
文献类型：
--
作者：
Rosenthal AS;Chen X;Liu JO;West DC;Hergenrother PJ;Shapiro TA;Posner GH
以天然三氧六环青蒿素为原料，经5或6步反应合成了新的6-二聚三氧环砜。其中一种热稳定性和水解性稳定的新化学物质(4c)通过单次口服144毫克/公斤即可完全治愈疟疾感染的小鼠。在低得多的单次口服剂量仅为54毫克/公斤和13毫克/公斤的盐酸甲氟喹的情况下，这种三氧六环二聚体4c及其母体三氧六环二聚体4b也完全治愈了疟疾感染的小鼠。二聚体4c和4b对5种癌细胞株均有较强的选择性细胞毒作用。
A new series of 6 dimeric trioxane sulfones has been prepared from the natural trioxane artemisinin in 5 or 6 chemical steps. One of these thermally and hydrolytically stable new chemical entities (4c) completely cured malaria-infected mice via a single oral dose of 144 mg/kg. At a much lower single oral dose of only 54 mg/kg combined with 13 mg/kg of mefloquine hydrochloride, this trioxane dimer 4c as well as its parent trioxane dimer 4b also completely cured malaria-infected mice. Both dimers 4c and 4b were potently and selectively cytotoxic toward five cancer cell lines.
登录
查看更多内容
影响因子：
7.3
作者：
Jung, M;Lee, S;Kim, SK
通讯作者：
Kim, SK
DOI：
10.3816/cgc.2002.n.005
发表时间：
2002-06-01
期刊：
Clinical prostate cancer
影响因子：
--
作者：
Harris, Katherine A;Harney, Elaine;Small, Eric J
通讯作者：
Small, Eric J
影响因子：
56.9
作者：
KLAYMAN, DL
通讯作者：
KLAYMAN, DL
影响因子：
3.4
作者：
GATTER, KC;BROWN, G;MASON, DY
通讯作者：
MASON, DY
影响因子：
16.6
作者：
Haynes, RK;Fugmann, B;Römer, A
通讯作者：
Römer, A