Abstract
A series of LXY3 (1) analogues were designed and synthesized. Their binding affinity was demonstrated using MDA-MB-231 breast cancer cells adherence inhibition assay. Further structure-activity relationship was obtained. Analogue 29 was discovered to have 3.5-fold increase of the binding affinity. Fluorescent microscopy and in vivo and ex vivo imaging studies demonstrated that 29 is an efficient in vivo targeting agent against α3 integrin of MDA-MB-231 breast tumor xenograft implant.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 6744-6751 |
| Number of pages | 8 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 52 |
| Issue number | 21 |
| DOIs | |
| State | Published - Nov 12 2009 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
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Cite this
Yao, N., Xiao, W., Meza, L., Tseng, H., Chuck, M., & Lam, K. (2009). Structure - Activity relationship studies of targeting ligands against breast cancer cells. Journal of Medicinal Chemistry, 52(21), 6744-6751. https://doi.org/10.1021/jm9012032