A Novel Kind of HIV-1 NNRTIs:From Natural Product Suksdorfinto Preclinical Candidates 3',4'

来源 :2006中国天津世界艾滋病日科技会议 | 被引量 : 0次 | 上传用户:hemir
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  Natural products are an important source to discover lead compounds and develop new drugs.In anti-HIV screening for plant natural products,suksdorfin (1) isolated from the fiuit of Lomatium suksdorfii lexhibited potent inhibitory activity against HIV-1 replication with an EC50 value of 1.3 mM in H9 lymphocytes.The modification ofsuksdorfm then found out a lead compound 3,4-.Di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK,2)2 with a remarkable EC50 value of 2.56× 10-4 M and a therapeutic index of 1.37× 105 in H9 lymphocytes,which was more potent than AZT (EC50 4.6×10-2 M and TI 10,000) in the same assay.
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