Publication: Synthesis and in vitro activities of new anticancer duplex drugs linking 2'-deoxy-5-fluorouridine (5-FdU) with 3'-C-ethynylcytidine (ECyd) via a phosphodiester bonding
Synthesis and in vitro activities of new anticancer duplex drugs linking 2'-deoxy-5-fluorouridine (5-FdU) with 3'-C-ethynylcytidine (ECyd) via a phosphodiester bonding
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Schott, H., Schott, S., & Schwendener, R. (2009). Synthesis and in vitro activities of new anticancer duplex drugs linking 2’-deoxy-5-fluorouridine (5-FdU) with 3’-C-ethynylcytidine (ECyd) via a phosphodiester bonding. Bioorganic & Medicinal Chemistry, 17(19), 6824–6831. https://doi.org/10.1016/j.bmc.2009.08.033
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Two isomeric cytostatic duplex drugs 2'-deoxy-5-fluorouridylyl-(3'-->5')-3'-C-ethynylcytidine [5-FdU(3'-->5')ECyd] and 2'-deoxy-5-fluorouridylyl-(5'-->5')-3'-C-ethynylcytidine [5-FdU(5'-->5')ECyd] were designed and synthesized at gram scale according to the hydrogenphosphonate method in an overall yield of about 40%. The in vitro evaluation of the anticancer effects indicated highly varying sensibilities of the panel of 60 tested tumor cell lines against the duplex drugs. 5-FdU(3'-->5')ECyd had a 50% growth inhibition (IC(50) < or = 1
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- Schott, H
- Schott, S
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Schott, H., Schott, S., & Schwendener, R. (2009). Synthesis and in vitro activities of new anticancer duplex drugs linking 2’-deoxy-5-fluorouridine (5-FdU) with 3’-C-ethynylcytidine (ECyd) via a phosphodiester bonding. Bioorganic & Medicinal Chemistry, 17(19), 6824–6831. https://doi.org/10.1016/j.bmc.2009.08.033
