Bioorg Med Chem Lett. 2011 Jun 15;21(12):3573-7. doi: 10.1016/j.bmcl.2011.04.106. Epub 2011 Apr 28.

Synthesis of substituted triazolyl curcumin mimics that inhibit RANKL-induced osteoclastogenesis.

Park SK, Oh S, Shin HK, Kim SH, Ham J, Song JS, Lee S.

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Department of Biochemistry, Kwandong University College of Medicine, Gangneung, Republic of Korea.

Abstract

Some promising new antiresorptive agents of potential utility for treating osteoporosis were uncovered in a curcumin mimics library possessing a substituted triazole moiety, which is synthesized by the Cu(I)-catalyzed Huisgen 1,3-cycloaddition reaction between two azido intermediates (9 and 10) and various alkynes (a-k). A tartarate-resistant acid phosphatase (TRAP) activity assay was carried out with RANKL-induced osteoclastogenesis of mouse monocyte/macrophage RAW264.7 cells; the results indicated that the curcumin mimics derived from intermediate 10 exhibited stronger inhibitory activity than 9. In particular, curcumin mimics 12h, 13c, and 13e strongly inhibited osteoclast differentiation.

PMID:: 21570847; [PubMed - indexed for MEDLINE]

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Synthesis of substituted triazolyl curcumin mimics that inhibit RANKL-induced os...
Synthesis of substituted triazolyl curcumin mimics that inhibit RANKL-induced osteoclastogenesis.
Bioorg Med Chem Lett. 2011 Jun 15 ;21(12):3573-7. doi: 10.1016/j.bmcl.2011.04.106. Epub 2011 Apr 28 .

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