271772-18-0Relevant academic research and scientific papers
Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): Synthesis and biological evaluation
Ferla, Salvatore,Aboraia, Ahmed S.,Brancale, Andrea,Pepper, Christopher J.,Zhu, Jinge,Ochalek, Justin T.,Deluca, Hector F.,Simons, Claire
, p. 7702 - 7715 (2015/01/08)
The synthesis of imidazole styrylbenzamide, tert-butyl styrylimidazole, and tert-butyl styrylsulfonate derivatives is described. Evaluation of binding affinity and inhibitory activity against CYP24A1 identified the imidazole styrylbenzamides as potent inhibitors of CYP24A1, having selectivity with respect to CYP27B1 comparable with or greater than that of the standard ketoconazole. Further evaluation of the 3,5-dimethoxy and 3,4,5-trimethoxy derivatives in chronic lymphocytic leukemia cells revealed that co-treatment of 1α,25-dihydroxyvitamin D3plus inhibitor coordinately upregulated GADD45α and CDKN1A. Docking experiments on the inhibitors in the CYP24A1 enzyme active site suggest the compounds reach the active site through the vitamin D access tunnel and are exposed to multiple hydrophobic residues. The imidazole styrylbenzamides are optimally positioned to allow interaction of the imidazole with the heme, and, in the case of the methoxy derivatives, a hydrogen bond between the 3-methoxy group and Gln82 stabilizes the molecule in a favorable active conformation.
Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARα
Mizuno, Cassia S.,Ma, Guoyi,Khan, Shabana,Patny, Akshay,Avery, Mitchell A.,Rimando, Agnes M.
, p. 3800 - 3808 (2008/09/21)
Pterostilbene, a naturally occurring analog of resveratrol, has previously shown PPARα activation in H4IIEC3 cells and was found to decrease cholesterol levels in animals. In this study, analogs of pterostilbene were synthesized and their ability to activ
PREVENTION AND TREATMENT OF COLON CANCER
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Page/Page column 25-26, (2008/12/06)
Stilbene compounds for the prevention and treatment of colon cancer or colon inflammation and methods of using same are provided.
