ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites
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- 作者：Sahar Kandila ; kandils1@cf.ac.uk" class="auth_mail" title="E-mail the corresponding author ; Jan Balzarinib ; Stephanie Rata ; Andrea Brancalea ; Andrew D. Westwella ; Christopher McGuigana
- 关键词：BVdU ; ProTide ; Phosphoramidate ; Anticancer ; Nucleoside ; Prodrug ; Brivudine
- 刊名：Bioorganic & Medicinal Chemistry Letters
- 出版年：2016
- 出版时间：1 December 2016
- 年：2016
- 卷：26
- 期：23
- 页码：5618-5623
- 全文大小：1058 K
文摘
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Synthesis of 46 BVdU ProTide derivatives with superior activity over BVdU.
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Anti-proliferative activity against L1210, CEM, HeLa and HEL cell lines.
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Up to 20-fold cytostatic activity enhancement over the parent BVdU.
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Retention or increase of the cytostatic activity against TK-deficient cancer cells.
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Separation of 4 pairs of P diastereoisomers and comparison of their properties.