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Synthesis and biological evaluation of novel C1 or C3 amino derivatives of A-ring 1,2,3-trisubstituted 19-nor-vitamin D3
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DOI：10.1016/j.bmc.2025.118523.png)
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Abstract
En 中文
• Two new analogs of 1α,25-dihydroxy-19-nor-vitamin D3 with an additional hydroxyl group at position 2 and an amino group at C1 or C3 are described. • Key step was the deprotection of the N-benzyl group mediated by an efficient biocatalytic system of Laccase from Trametes versicolor together with TEMPO. • The synthesized analogs did not exhibit any significant affinity for binding to either the VDR or hDBP when compared to the natural hormone and 1α,25-dihydroxy-19-nor-vitamin D3. • In terms of their antiproliferative activity in MCF-7 and HL-60 cells, the reported influence of the hydroxyl group at C1 on biological activity of vitamin D analogs is observed.
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B
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3
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1.7W
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