18 research outputs found
Structural Evaluation of the Agonistic Action of a Vitamin D Analog with Two Side Chains Binding to the Nuclear Vitamin D Receptor
1,25-(OH)2-16ene-23yne-D3 reduces secondary hyperparathyroidism in uremic rats with little calcemic effect
To compare the effects of vitamin D analogs versus calcitriol on serum levels of Ca, P and parathyroid hormone (PTH). A compound better than calcitriol should increase the Ca x P product less than calcitriol for an equivalent decrease in PTH levels
Diastereotopic and Deuterium Effects in Gemini
Changing the geminal methyl groups
on 1α,25-dihydroxyvitamin
D<sub>3</sub> and its analogues to the deuterio versions generally
improves the bioactivity. Derivatives of 1α,25-dihydroxyvitamin
D<sub>3</sub> with two chains emanating at C20, commonly referred
to as gemini, are subject to the same phenomenon. Additionally, gemini
with different side chains are susceptible to bioactivity differentials
where the C17–C20 threo configuration usually imparts higher
activity than the corresponding erythro arrangement. In an effort
to analyze the deuterium effect on gemini with minimal diastereotopic
distortion, we synthesized gemini with equal side chains but introduced
deuterium diastereospecifically on either chain. We solved the crystal
structures of these compounds in the zebra fish zVDR ligand binding
domain as complexes with NCoA-2 coactivator peptide and correlated
the findings with growth inhibition in a breast cancer cell line
Calcitriol derivatives with two different side-chains at C-20. Part 4: Further chain modifications that alter VDR-dependent monocytic differentiation potency in human leukemia cells
Synergistic Antileukemic Activity of Carnosic Acid-Rich Rosemary Extract and the 19-nor Gemini Vitamin D Analogue in a Mouse Model of Systemic Acute Myeloid Leukemia
Novel Gemini vitamin D3 analogs:large structure/function analysis and ability to induce antimicrobial peptide
10.1002/ijc.28328International Journal of Cancer1341207-217IJCN