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 |
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ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
Cite this
Structure - Activity relationship studies of targeting ligands against breast cancer cells. / Yao, Nianhuan; Xiao, Wenwu; Meza, Leah; Tseng, Harry; Chuck, Mathida; Lam, Kit.
In: Journal of Medicinal Chemistry, Vol. 52, No. 21, 12.11.2009, p. 6744-6751.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Structure - Activity relationship studies of targeting ligands against breast cancer cells
AU - Yao, Nianhuan
AU - Xiao, Wenwu
AU - Meza, Leah
AU - Tseng, Harry
AU - Chuck, Mathida
AU - Lam, Kit
PY - 2009/11/12
Y1 - 2009/11/12
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=71049195364&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=71049195364&partnerID=8YFLogxK
U2 - 10.1021/jm9012032
DO - 10.1021/jm9012032
M3 - Article
VL - 52
SP - 6744
EP - 6751
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 21
ER -