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The UVB1 Vitamin D Analogue Inhibits Colorectal Carcinoma Progression
(Pergamon-Elsevier Science Ltd, 2016-10)
Vitamin D has been shown to display a wide variety of antitumour effects, but their therapeutic use is limited by its severe side effects. We have designed and synthesized a Gemini vitamin D analogue of calcitriol (UVB1) ...
Synthesis of 1α,25-Dihydroxyvitamin D3 Analogues with α-Hydroxyalkyl Substituents at C12
(2013)
Convergent syntheses of three new analogues of 1α,25-dihydroxyvitamin D3 with α-hydroxyalkyl substituents at C12 (4a–c) are described. The A-ring and triene system of each analogue were assembled by a tandem Pd-catalysed ...
Novel calcitriol analogue with an oxolane group: In vitro, in vivo, and in silico studies
(Wiley VCH Verlag, 2019-04-26)
The active form of vitamin D3, calcitriol, is a potent antiproliferative compound. However, when effective antitumor doses of calcitriol are used, hypercalcemic effects are observed, thus blocking its therapeutic application. ...
The alkynylphosphonate analogue of calcitriol EM1 has potent anti-metastatic effects in breast cancer
(Pergamon-elsevier Science Ltd, 2015-09)
The active form of vitamin D3, calcitriol, plays a major role in maintaining calcium/phosphate homeostasis. In addition, it is a potent antiproliferative and prodifferentiating agent. However, when effective antitumor doses ...
Monitoring chemical and biological electron transfer reactions with a fluorogenic vitamin K analogue probe
(American Chemical Society, 2016-12)
We report herein the design, synthesis, and characterization of a two-segment fluorogenic analogue of Vitamin K, B-VKQ, prepared by coupling Vitamin K3, also known as menadione (a quinone redox center), to a boron-dipyrromethene ...
Vitamin D analogues exhibit antineoplastic activity in breast cancer patient-derived xenograft cells
(Pergamon-Elsevier Science Ltd, 2020-08-09)
Despite advances in breast cancer (BC) treatment, its mortality remains high due to intrinsic or acquired resistance to therapy. Several ongoing efforts are being made to develop novel drugs to treat this pathology with ...
Synthesis, structure, and biological activity of des-side Chain analogues of 1α,25-Dihydroxyvitamin D3 with substituents at C18
(Wiley VCH Verlag, 2011-05)
An improved synthetic route to 1α,25-dihydroxyvitamin D3 des-side chain analogues 2a and 2b with substituents at C18 is reported, along with their biological activity. These analogues display significant antiproliferative ...
Vitamin D receptor exhibits different pharmacodynamic features in tumoral and normal microenvironments: A molecular modeling study
(Pergamon-Elsevier Science Ltd, 2020-03-03)
The vitamin D receptor (VDR) constitutes a promising therapeutic target for the treatment of cancer. Unfortunately, its natural agonist calcitriol does not have clinical utility due to its potential to induce hypercalcemic ...