Literature DB >> 15482941

Synthesis and CYP24 inhibitory activity of 2-substituted-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives.

Sook Wah Yee1, Claire Simons.   

Abstract

The synthesis of novel 2-benzyl- and 2-benzylidene-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives and their inhibitory activity versus kidney mitochondrial 25-hydroxyvitamin D(3) 24-hydroxylase (CYP24) is described. The 2-benzylidenetetralone derivatives were found to be very weak inhibitors (IC(50) 20 >100 microM), whereas the 2-benzyltetralone derivatives showed promising inhibitory activity (IC(50) 0.9 microM for the most active derivative) compared with ketoconazole (IC(50) 20 microM).

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Year:  2004        PMID: 15482941     DOI: 10.1016/j.bmcl.2004.08.040

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  9 in total

1.  Synthesis and biological activities of vitamin D-like inhibitors of CYP24 hydroxylase.

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Journal:  Steroids       Date:  2011-11-25       Impact factor: 2.668

2.  A local effect of CYP24 inhibition on lung tumor xenograft exposure to 1,25-dihydroxyvitamin D(3) is revealed using a novel LC-MS/MS assay.

Authors:  Jan H Beumer; Robert A Parise; Beatriz Kanterewicz; Martin Petkovich; David Z D'Argenio; Pamela A Hershberger
Journal:  Steroids       Date:  2012-01-20       Impact factor: 2.668

Review 3.  24-Hydroxylase in cancer: impact on vitamin D-based anticancer therapeutics.

Authors:  Wei Luo; Pamela A Hershberger; Donald L Trump; Candace S Johnson
Journal:  J Steroid Biochem Mol Biol       Date:  2012-10-08       Impact factor: 4.292

Review 4.  Human cytochrome P450 enzymes 5-51 as targets of drugs and natural and environmental compounds: mechanisms, induction, and inhibition - toxic effects and benefits.

Authors:  Slobodan P Rendic; F Peter Guengerich
Journal:  Drug Metab Rev       Date:  2018-08       Impact factor: 4.518

5.  Synthesis of benzyl substituted naphthalenes from benzylidene tetralones.

Authors:  Lorraine M Deck; Quintino Mgani; Andrea Martinez; Alice Martinic; Lisa J Whalen; David L Vander Jagt; Robert E Royer
Journal:  Tetrahedron Lett       Date:  2012-01-25       Impact factor: 2.415

6.  Combination of calcitriol and dietary soy exhibits enhanced anticancer activity and increased hypercalcemic toxicity in a mouse xenograft model of prostate cancer.

Authors:  Jennifer Y Wang; Srilatha Swami; Aruna V Krishnan; David Feldman
Journal:  Prostate       Date:  2012-03-27       Impact factor: 4.104

7.  Benzylidene-6-hydroxy-3,4-dihydronaphthalenone chalconoids as potent tyrosinase inhibitors.

Authors:  Sara Ranjbar; Mehraneh Mohammadabadi Kamarei; Mahsima Khoshneviszadeh; Hona Hosseinpoor; Najmeh Edraki; Mehdi Khoshneviszadeh
Journal:  Res Pharm Sci       Date:  2021-06-30

Review 8.  Vitamin D in prostate cancer.

Authors:  Donald L Trump; Jeanny B Aragon-Ching
Journal:  Asian J Androl       Date:  2018 May-Jun       Impact factor: 3.285

9.  Calcitriol and cancer therapy: A missed opportunity.

Authors:  Donald L Trump
Journal:  Bone Rep       Date:  2018-06-13
  9 in total

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