NDLI: Small molecules inhibit ex vivo tumor growth in bone

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Small molecules inhibit ex vivo tumor growth in bone

Content Provider	Scilit
Author	Zhou, Donghui Bum-Erdene, Khuchtumur Xu, David Liu, Degang Tompkins, Doug Sulaiman, Rania S. Corson, Timothy W. Chirgwin, John M. Meroueh, Samy O.
Copyright Year	2018
Description	Journal: Bioorganic & Medicinal Chemistry Bone is a common site of metastasis for breast, prostate, lung, kidney and other cancers. Bone metastases are incurable, and substantially reduce patient quality of life. To date, there exists no small-molecule therapeutic agent that can reduce tumor burden in bone. This is partly attributed to the lack of suitable in vitro assays that are good model of tumor growth in bone. Here, we take advantage of a novel ex vivo model of bone colonization to report a series of pyrrolopyrazolone small molecules that inhibit cancer cell invasion and ex vivo tumor growth in bone at single-digit micromolar concentration. We find that the compounds modulated the expression levels of genes associated with bone-forming osteoblasts, bone-destroying osteoclasts, cancer cell viability and metastasis. Our compounds provide chemical tools to uncover novel targets and pathways associated with bone metastasis, as well as for the development of compounds to prevent and reverse bone tumor growth in vivo.
Related Links	https://scholarworks.iupui.edu/bitstream/1805/18009/1/Zhou_2018_small.pdf
Ending Page	6134
Page Count	7
Starting Page	6128
ISSN	09680896
e-ISSN	14643391
DOI	10.1016/j.bmc.2018.11.025
Journal	Bioorganic & Medicinal Chemistry
Issue Number	23-24
Volume Number	26
Language	English
Publisher	Elsevier BV
Publisher Date	2018-11-16
Access Restriction	Open
Subject Keyword	Journal: Bioorganic & Medicinal Chemistry Medicinal Chemistry Quality of Life Small Molecule
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Drug Discovery Biochemistry Clinical Biochemistry Molecular Biology Molecular Medicine Pharmaceutical Science

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