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• W2106546968 abstract "A series of 2′,3′-bis-O-silylated or -acylated derivatives of lead compound 3a (2′,3′-bis-O-tert-butyldimethylsilyl-5′-deoxy-5′-(N-methylcarbamoyl)amino-N6-(N-phenylcarbamoyl)adenosine) were prepared and evaluated for antiproliferative activity against a panel of murine and human cancer cell lines (L1210, FM3A, CEM, and HeLa). 2′,3′-O-Silyl groups investigated included triethylsilyl (10a), tert-butyldiphenylsilyl (10b), and triisopropylsilyl (10c). 2′,3′-O-Acyl groups investigated included acetyl (13a), benzoyl (13b), isobutyryl (13c), butanoyl (13d), pivaloyl (13e), hexanoyl (13f), octanoyl (13g), decanoyl (13h), and hexadecanoyl (13i). IC50 values ranged from 3.0 ± 0.3 to >200 μg/mL, with no improvement relative to lead compound 3a. Derivative 10a was approximately equipotent to 3a, while compounds 13e–g were from three to fivefold less potent, and all other compounds were significantly much less active. A desilylated derivative (5′-deoxy-5′-(N-methylcarbamoyl)amino-N6-(N-phenylcarbamoyl)adenosine; 5) and several representative derivatives from each subgroup (10a–10c, 13a–13c) were screened for binding affinity for bone morphogenetic protein receptor 1b (BMPR1b). Only compound 5 showed appreciable affinity (Kd = 11.7 ± 0.5 μM), consistent with the inference that 3a may act as a prodrug depot form of the biologically active derivative 5. Docking studies (Surflex Dock, Sybyl X 1.3) for compounds 3a and 5 support this conclusion." @default.
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• W2106546968 date "2012-10-01" @default.
• W2106546968 modified "2023-10-16" @default.
• W2106546968 title "Synthesis and SAR of 2′,3′-bis-O-substituted N6, 5′-bis-ureidoadenosine derivatives: Implications for prodrug delivery and mechanism of action" @default.
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• W2106546968 doi "https://doi.org/10.1016/j.bmcl.2012.08.050" @default.
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