- A systematic study on the use of different organocatalytic activation modes for asymmetric conjugated addition reactions of isoindolinones
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In this article we describe a series of new asymmetric Michael reactions of carboxylate-3-substituted isoindolinones used as nucleophiles in the synthesis of valuable chiral tetrasubstituted derivatives. It has been shown that the reactivity and enantiose
- Scorzelli, Francesco,Di Mola, Antonia,De Piano, Francesco,Tedesco, Consiglia,Palombi, Laura,Filosa, Rosanna,Waser, Mario,Massa, Antonio
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supporting information
p. 819 - 828
(2017/01/28)
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- Design, synthesis and biological evaluation of 3-substituted indenoisoquinoline derivatives as topoisomerase I inhibitors
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A new series of indenoisoquinoline derivatives was designed and synthesized. The in vitro anti-proliferative activity of these novel compounds was evaluated in HepG2, A549 and HCT-116 cell lines. Compounds 9a, 9b, 10a, 10c, 10e, 18a and 18b manifested potent inhibitory activity against the three tested cancer cell lines. Nineteen compounds were also tested for Top I inhibition at 50 μM. Almost all the tested compounds showed potent Top I inhibition activity at this concentration. The most potent compounds 9a and 10a demonstrated more cytotoxicity than HCPT and TPT and was comparable to CPT in inhibitory activities on Top I in our biological assay.
- Zhao, Qian,Xu, Xi,Xie, Zhouling,Liu, Xiao,You, Qidong,Guo, Qinglong,Zhong, Yi,Li, Zhiyu
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supporting information
p. 1068 - 1072
(2016/05/24)
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- Total synthesis and anti-viral activities of an extract of radix isatidis
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Radix isatidis (Banlangen), a famous traditional Chinese medicine, has been used for thousands of years in China due to its anti-viral activity. Through our research, we inferred that the anti-viral activity of Radix isatidis depended on the water-soluble
- He, Li-Wei,Chen, Yu-Qing,Yang, Jing-Yan,Wang, Tian-Lin,Li, Wei,Liu, Hua-Qing
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p. 20906 - 20912
(2015/03/04)
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- 2-HYDROXYISOQUINOLINE-1,3(2H,4H)-DIONES AND RELATED COMPOUNDS USEFUL AS HIV REPLICATION INHIBITORS
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The present invention relates to compounds and compositions acting as inhibitors of HIV integrase. The compound of the invention is of Formula (I), or a tautomer (I') thereof, or a pharmaceutically acceptable salt, or solvate of said compound or tautomer
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Page/Page column 112-113
(2012/07/13)
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- Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain
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We report herein the synthesis of a series of 19 2-hydroxyisoquinoline-1, 3(2H,4H)-dione derivatives variously substituted at position 7 aimed at inhibiting selectively two-metal ion catalytic active sites. The compounds were tested against HIV-1 reverse
- Billamboz, Muriel,Bailly, Fabrice,Barreca, Maria Letizia,De Luca, Laura,Mouscadet, Jean-Fran?ois,Calmels, Christina,Andréola, Marie-Line,Witvrouw, Myriam,Christ, Frauke,Debyser, Zeger,Cotelle, Philippe
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experimental part
p. 7717 - 7730
(2009/12/07)
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