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Water-soluble Withaferin A polymer prodrugs via a drug-functionalized RAFT CTA approach

(2019) EUROPEAN POLYMER JOURNAL. 110. p.313-318
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Abstract
To cope with the poor aqueous solubility of withaferin A, a broad-spectrum anti-cancer agent effective against therapy-resistant cancers, a polymer-drug conjugate was synthesized via a grafting-from-drug approach. Modification of withaferin A at the C27-OH with a chain transfer agent (CTA) for reversible addition-fragmentation chain transfer (RAFT) polymerization through a degradable ester bond was achieved with excellent control on the regioselectivity via a PFP-ester transesterification route. Subsequent RAFT polymerization with the hydrophilic N,N-dimethylacrylamide yielded a fully water-soluble conjugate. A decreased cytotoxicity in vitro indicated that withaferin A exists as a prodrug in the conjugate form and requires hydrolysis of the ester to regain its activity.
Keywords
Withaferin A, Polymer conjugate

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Chicago
Van Herck, Simon, Behrouz Hassannia, Benoit Louage, Raquel Pita Compostizo, Ruben De Coen, Wim Vanden Berghe, Tom Vanden Berghe, and Bruno De Geest. 2019. “Water-soluble Withaferin A Polymer Prodrugs via a Drug-functionalized RAFT CTA Approach.” European Polymer Journal 110: 313–318.
APA
Van Herck, S., Hassannia, B., Louage, B., Pita Compostizo, R., De Coen, R., Vanden Berghe, W., Vanden Berghe, T., et al. (2019). Water-soluble Withaferin A polymer prodrugs via a drug-functionalized RAFT CTA approach. EUROPEAN POLYMER JOURNAL, 110, 313–318.
Vancouver
1.
Van Herck S, Hassannia B, Louage B, Pita Compostizo R, De Coen R, Vanden Berghe W, et al. Water-soluble Withaferin A polymer prodrugs via a drug-functionalized RAFT CTA approach. EUROPEAN POLYMER JOURNAL. 2019;110:313–8.
MLA
Van Herck, Simon et al. “Water-soluble Withaferin A Polymer Prodrugs via a Drug-functionalized RAFT CTA Approach.” EUROPEAN POLYMER JOURNAL 110 (2019): 313–318. Print.
@article{8583641,
  abstract     = {To cope with the poor aqueous solubility of withaferin A, a broad-spectrum anti-cancer agent effective against therapy-resistant cancers, a polymer-drug conjugate was synthesized via a grafting-from-drug approach. Modification of withaferin A at the C27-OH with a chain transfer agent (CTA) for reversible addition-fragmentation chain transfer (RAFT) polymerization through a degradable ester bond was achieved with excellent control on the regioselectivity via a PFP-ester transesterification route. Subsequent RAFT polymerization with the hydrophilic N,N-dimethylacrylamide yielded a fully water-soluble conjugate. A decreased cytotoxicity in vitro indicated that withaferin A exists as a prodrug in the conjugate form and requires hydrolysis of the ester to regain its activity.},
  author       = {Van Herck, Simon and Hassannia, Behrouz and Louage, Benoit and Pita Compostizo, Raquel and De Coen, Ruben and Vanden Berghe, Wim and Vanden Berghe, Tom and De Geest, Bruno},
  issn         = {0014-3057},
  journal      = {EUROPEAN POLYMER JOURNAL},
  language     = {eng},
  pages        = {313--318},
  title        = {Water-soluble Withaferin A polymer prodrugs via a drug-functionalized RAFT CTA approach},
  url          = {http://dx.doi.org/10.1016/j.eurpolymj.2018.11.043},
  volume       = {110},
  year         = {2019},
}

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