Structure - Activity relationship studies of targeting ligands against breast cancer cells

Nianhuan Yao; Wenwu Xiao; Leah Meza; Harry Tseng; Mathida Chuck; Kit Lam

doi:10.1021/jm9012032

Structure - Activity relationship studies of targeting ligands against breast cancer cells

Nianhuan Yao, Wenwu Xiao, Leah Meza, Harry Tseng, Mathida Chuck, Kit Lam

Research output: Contribution to journal › Article

12 Scopus citations

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	https://doi.org/10.1021/jm9012032
State	Published - Nov 12 2009

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ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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

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10.1021/jm9012032