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Synthesis of New Conjugates of Modified Podophyllotoxin and Stavudine
Authors:Shi‐Wu Chen  Rong Xiang  Xuan Tian
Affiliation:1. School of Pharmacy, Lanzhou University, Lanzhou 730000, P.?R. China, (phone/fax: +86‐931‐8915686);2. State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, P.?R. China;3. Lanzhou Hospital of Traditional Chinese Medicine Traumatocomium, Lanzhou 730000, P.?R. China
Abstract:To find podophyllotoxin compounds with superior bioactivitiy and less toxicity, a series of novel conjugates of ring‐A‐modified 4‐epipodophyllotoxin and stavudine with amino acids as spacers were synthesized, i.e., the N‐[(2′,3′‐didehydro‐3′‐deoxythymidin‐5′‐O‐yl)carbonyl]‐substituted L ‐amino acid rel‐(3aR,4S,9R,9aR)‐1,3,3a,4,9,9a‐hexahydro‐6,7‐dimethoxy‐1‐oxo‐9‐(3,4,5‐trimethoxyphenyl)naphtho[2,3‐c]furan‐4‐yl esters 8a – 8f .
Keywords:Podophyllotoxin  Stavudine  Amino acids  Antiviral activity  Anti‐HIV activity
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