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Kazuki Shimizu et al.
Bioorganic & medicinal chemistry letters, 16(12), 3323-3329 (2006-04-25)
Design, synthesis, and in vitro and in vivo evaluation of a series of antipsoriatic antedrugs having 16-en-22-oxa-vitamin D3 are described. Among the seven compounds examined, two are promising: ester 5c and amide 5f, both of which exhibit greater potent antiproliferation...
Marc Lamblin et al.
Bioorganic & medicinal chemistry, 18(11), 4119-4137 (2010-05-11)
Incorporation of zinc-binding groups into the side-chain of 1alpha,25-dihydroxyvitamin D(3) (1,25D) fully bifunctional hybrid molecules which act both as vitamin D receptor agonists and histone deacetylase inhibitors. These bifunctional hybrids display in vitro antiproliferative activity against the AT84 squamous carcinoma...
Maria A Regueira et al.
Journal of medicinal chemistry, 54(11), 3950-3962 (2011-04-29)
We designed by docking and synthesized two novel analogues of 1α,25-dihydroxyvitamin D(3) hydroxymethylated at C-26 (2 and 3). The syntheses were carried out by the convergent Wittig-Horner approach via epoxide 12a as a common key intermediate. The antiproliferative and transactivation...
Su'e Chang et al.
Oncotarget, 6(10), 7675-7685 (2015-03-13)
VitaminD3 signaling is involved in inhibiting the development and progression of gastric cancer (GC), while the active vitamin D metabolite 1-alpha,25-dihydroxyvitamin D3 (1,25(OH)2D3)-mediated gene regulatory mechanisms in GC remain unclear. We found that miR-145 is induced by 1,25(OH)2D3 in a...
Rafal Barycki et al.
Bioorganic & medicinal chemistry, 17(22), 7658-7669 (2009-10-13)
The 18-nor (7), 21-nor (8) and 18,21-dinor (9) analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D(3) (6, 2MD) were prepared by convergent syntheses. The known phosphine oxide 10 was coupled by the Wittig-Horner process with the corresponding C,D-fragments (13-15), obtained by a multi-step procedure...
Keiko Yamamoto et al.
Journal of medicinal chemistry, 50(5), 932-939 (2007-02-15)
We previously reported that 22R-methyl-20-epi-1,25-(OH)2D3 (3) possesses strong binding affinity for the vitamin D receptor (VDR) and shows superagonistic biological activities. To examine the effect of the length of an alkyl substituent at C(22) and to extend our compound library...
Zhixia Song et al.
Metabolism: clinical and experimental, 63(10), 1324-1333 (2014-07-22)
The present study aimed to investigate the relationship between PI3K/p-Akt signaling pathway and podocyte impairment in DN rats as well as the protective effect of calcitriol. SD rats were randomly divided into four groups: normal control (NC), normal treated with...
Xiao-Liang Zhang et al.
Endocrinology, 155(12), 4939-4950 (2014-09-05)
Increasing evidence suggests the heterogeneity of macrophage phenotype and function ultimately determines the outcome of diabetic nephropathy (DN). This study aimed to investigate the effects of vitamin D on macrophage M1/M2 phenotype and its role in preventing podocyte impairment in...
Masato Shimizu et al.
Bioorganic & medicinal chemistry, 16(14), 6949-6964 (2008-06-10)
Recently, we have found that 16-ene-22-thia-26,27-dimethyl-19-norvitamin D(3) analogs 1a (n=2, 3) are 20 times more active than the natural hormone 1alpha,25-dihydroxyvitamin D(3) in terms of transcriptional activity. To further investigate the effects of the A-ring modification of 1a, b on...
Taku Toriumi et al.
Biomedical research (Tokyo, Japan), 36(1), 31-45 (2015-03-10)
The existence of progenitor/mesenchymal stem cells (MSCs) was demonstrated previously in human primary/deciduous teeth. In this study, we examined dental pulp cells from root portion (root cells) of primary teeth without discernible root resorption and compared them with pulp cells...
Sara Peleg et al.
Journal of medicinal chemistry, 49(25), 7513-7517 (2006-12-08)
Replacing the 1alpha-OH group of the natural hormone 1alpha,25-dihydroxyvitamin D(3) (calcitriol) by a 1alpha-CHF(2) group and incorporating a potentiating side chain produced two new hybrid analogs 6 and 7. Both of these two hybrid analogs are as transcriptionally active as...
Agnieszka Glebocka et al.
Journal of medicinal chemistry, 54(19), 6832-6842 (2011-09-10)
As a continuation of our efforts directed to vitamin D compounds of promising biological properties, 19-norvitamins 9-13, possessing a 3'-hydroxypropylidene fragment attached to C-2 and shortened 17β-alkyl chains, were synthesized. A new synthetic pathway providing the CD-ring ketones 20-24 is...
Z L Zhang et al.
Osteoporosis international : a journal established as result of cooperation between the European Foundation for Osteoporosis and the National Osteoporosis Foundation of the USA, 26(9), 2365-2374 (2015-05-02)
This study compares efficacy of ALN/D5600 versus that of calcitriol in osteoporotic Chinese postmenopausal women. ALN/D5600 produced greater bone mineral density (BMD) increases, greater bone turnover marker decreases, and less vitamin D insufficiency. This study provided detailed clinical information regarding...
Agnieszka Glebocka et al.
Journal of medicinal chemistry, 52(11), 3496-3504 (2009-05-01)
Vitamin D compounds possessing A rings prohibited from flipping to the alternative chair form (i.e., analogues 2 and 26) were synthesized. The bicyclic fragment 22 consisting of the fused cyclohexane and dihydropyran rings was constructed via the ring-closing metathesis route....
Ling-Feng Wang et al.
The Kaohsiung journal of medical sciences, 31(2), 63-69 (2015-02-04)
Eosinophils are important inflammatory cells involved in the pathogenesis of chronic rhinosinusitis with nasal polyps (CRSwNP). Vitamin D and its derivatives, in addition to their classic role as regulators of electrolytes homeostasis, have modulatory effects in immunological and inflammatory responses....
K Afsal et al.
Tuberculosis (Edinburgh, Scotland), 94(6), 599-605 (2014-12-03)
1,25-dihydroxy vitamin D3 (1,25(OH)2D3) is a potent immuno-modulator which induces LL-37, the active peptide of cathelicidin, and restricts the growth of Mycobacterium tuberculosis (Mtb) in human macrophages. In the present study, we investigated the effect of 1,25(OH)2D3 on cathelicidin antimicrobial...
Nancy Noyola-Martínez et al.
The Journal of steroid biochemistry and molecular biology, 144 Pt A, 106-109 (2013-12-24)
Placenta is an important source of endocrine and immunological factors. During pregnancy, calcitriol, the active metabolite of vitamin D, is also metabolized by decidua and placental tissue by means of CYP27B1 and CYP24A1 for synthesis and inactivation of calcitriol respectively....
Marc Lamblin et al.
Journal of medicinal chemistry, 53(20), 7461-7465 (2010-10-05)
Vitamin D receptor (VDR) antagonists have therapeutic potential in treatment of allergic conditions and hypercalcemia driven by granulomatous diseases. We have identified an o-aminoanilide analogue of the hormonal form of vitamin D with a dienyl side chain that functions as...
Hubert Maehr et al.
Journal of medicinal chemistry, 52(17), 5505-5519 (2009-08-19)
Calcitriol is implicated in many cellular functions including cellular growth and differentiation, thus explaining its antitumor effects. It was shown that gemini, the calcitriol derivative containing two side chain at C20, is also active in gene transcription with enhanced antitumor...
Angsuma Wongmayura et al.
Bioorganic & medicinal chemistry letters, 22(4), 1756-1760 (2012-01-31)
Vitamin D receptor (VDR) is a nuclear receptor for 1α,25-dihydroxyvitamin D(3) (1α,25(OH)(2)D(3)), and is an attractive target for multiple clinical applications. We recently developed novel non-secosteroidal VDR ligands bearing a hydrophobic p-carborane cage, thereby establishing the utility of this spherical...
Pierre Antony et al.
Journal of medicinal chemistry, 53(3), 1159-1171 (2010-01-15)
The vitamin D nuclear receptor is a ligand-dependent transcription factor that controls multiple biological responses such as cell proliferation, immune responses, and bone mineralization. Numerous 1 alpha,25(OH)(2)D(3) analogues, which exhibit low calcemic side effects and/or antitumoral properties, have been synthesized....
Andrea Polistena et al.
International journal of surgery (London, England), 21, 128-134 (2015-08-09)
Prognosis of thyroid cancer is strictly related to loco-regional metastases. Cervical lymphadenectomy has a specific oncologic role but may lead to significant increase of morbidity. Aim of the study is the analysis of surgical morbidity in cervical lymphadenectomy for thyroid...
Kimberly S Petersen et al.
Journal of medicinal chemistry, 50(23), 5824-5832 (2007-10-11)
Eight new side-chain allylic, benzylic, and propargylic ether analogs of the natural hormone calcitriol have been rationally designed and easily synthesized. Three of these 23-oxa ether analogs lacking the typical side-chain OH group are more antiproliferative in vitro and desirably...
Rahul Ray et al.
Bioorganic & medicinal chemistry letters, 21(8), 2537-2540 (2011-03-12)
Synthesis of 1α,25-dihydroxyvitamin D(3)-3β-bromoacetate (1,25(OH)(2)D(3)-3-BE), a potential anti-cancer agent is presented. We also report that mechanism of action of 1,25(OH)(2)D(3)-3-BE may involve reduction of its catabolism, as evidenced by the reduced and delayed expression of 1α,25-dihydroxyvitamin D(3)-24-hydroxylase (CYP24) gene in...
Ghaith Bakdash et al.
Vaccine, 32(47), 6294-6302 (2014-09-23)
Vitamin D is recognized as a potent immunosuppressive drug. The suppressive effects of vitamin D are attributed to its physiologically active metabolite 1,25 dihydroxy vitamin D3 (calcitriol), which was shown, to prime dendritic cells (DCs) to promote the development of...
Ela Haddur et al.
Biochemistry and cell biology = Biochimie et biologie cellulaire, 93(3), 268-271 (2015-04-29)
Calcitriol, the active form of vitamin D, is known for its anticancer properties including induction of apoptosis, inhibition of angiogenesis, and metastasis. Calcitriol also increases intracellular calcium triggering apoptosis in a calpain-dependent manner. Since the main storage unit for cellular...
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this...
Francesca Tentori et al.
Clinical journal of the American Society of Nephrology : CJASN, 10(1), 98-109 (2014-12-18)
Elevated parathyroid hormone levels may be associated with adverse clinical outcomes in patients on dialysis. After the introduction of practice guidelines suggesting higher parathyroid hormone targets than those previously recommended, changes in parathyroid hormone levels and treatment regimens over time...
Rafal R Sicinski et al.
Journal of medicinal chemistry, 50(24), 6154-6164 (2007-10-27)
To establish the conformation of vitamin D compounds responsible for biological activity, a 1alpha,25-dihydroxy-19-norvitamin D analogue 4 possessing a 1alpha-hydroxy group fixed in the axial orientation (beta-chair form) was synthesized. The starting compounds were bicyclic lactones 6, 7a, and 7b...
Wataru Hakamata et al.
Bioorganic & medicinal chemistry letters, 18(1), 120-123 (2007-12-07)
Vitamin D receptor (VDR) ligands are therapeutic agents for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism. VDR ligands also show immense potential as therapeutic agents for autoimmune diseases and cancers of the skin, prostate, colon, and breast as well...
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