- 11-Aza-artemisinin Derivatives Exhibit Anticancer Activities by Targeting the Fatty Acid Binding Protein 6 (FABP6)
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Artemisinin (Qinghaosu), a sesquiterpene lactone isolated from the Chinese medicinal herb Artemisia annua, is famous as the first-line antimalarial drug, and reported to also possess anticancer properties. Though many studies have proceeded focusing on ar
- Chen, Xin-Ya,Yin, Yue,Xi, Jie,Yuan, Yi,Li, Yan,Li, Qing,Wang, Ren-Xiao,Yao, Zhu-Jun,Tang, Gong-Li
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- New orally active amino- and hydroxy-functionalized 11-azaartemisinins and their derivatives with high order of antimalarial activity against multidrug-resistant Plasmodium yoelii in swiss mice1
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By use of artemisinin 1 as the starting material, two new amino- and hydroxy-functionalized 11-azaartemisinins 9 and 11 and their derivatives 12a-g, 13a-g, 14a-g, and 15a-c have been prepared and screened for antimalarial activity by oral route against mu
- Singh, Chandan,Verma, Ved Prakash,Hassam, Mohammad,Singh, Ajit Shankar,Naikade, Niraj K.,Puri, Sunil K.
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p. 2489 - 2497
(2014/04/17)
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- Amino- and hydroxy-functionalized 11-azaartemisinins and their derivatives
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(Chemical Equation Presented) An efficient conversion of artemisinin 1 into three new amino- and hydroxy-functionalized 11-aza prototypes 9, 11, and 12 has been achieved on a multigram scale by reaction with hydrazine, hydroxylamine, and 2-amino ethanol, respectively. Of these, 9 has been further diversified into a wide range of derivatives including imines, amines, amides, and linker based dimers. Prototypes 11 and 12 have been converted into the corresponding ethers in high yields. Some of these compounds have shown a high order of activity against multidrug-resistant malaria in mice by oral route.
- Singh, Ajit Shankar,Verma, Ved Prakash,Hassam, Mohammad,Krishna, Naikade Niraj,Puri, Sunil K.,Singh, Chandan
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supporting information; experimental part
p. 5461 - 5464
(2009/06/06)
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