(-)-Arctigenin as a lead structure for inhibitors of human immunodeficiency virus type-1 integrase

…, H Pertz, M Kaloga, J Schulz, MR Fesen…

文献索引：Eich, Eckart; Pertz, Heinz; Kaloga, Macki; Schulz, Jutta; Fesen, Mark R.; Mazumder, Abhijit; Pommier, Yves Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 86 - 95

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被引用次数: 222

摘要

The natural dibenzylbutyrolactone type lignanolide (-)-arctigenin (2), an inhibitor of human immunodeficiency virus type-1 (HIV-1) replication in infected human cell systems, was found to suppress the integration of proviral DNA into the cellular DNA genome. 11b In the present study 2 was tested with purified HIV-1 integrase and found to be inactive in the cleavage (3'- processing) and integration (strand transfer) assays. However, the semisynthetic 3-O- ...