- Title
-
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines that Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase
- Authors
- Fraser, C., Dawson, J.C., Dowling, R., Houston, D.R., Weiss, J.T., Munro, A.F., Muir, M., Harrington, L., Webster, S.P., Frame, M.C., Brunton, V.G., Patton, E.E., Carragher, N.O., Unciti-Broceta, A.
- Source
- Full text @ J. Med. Chem.
(a,b) Neuromast migration assay. Fresh E3 media with DMSO or 11a (500 µM) was added to zebrafish embryos at 20 hpf, 36 hpf, and 48 hpf and imaged at 72 hpf. (a) Representative images of the tail of a 3 dpf zebrafish without (top) and with 11a treatment (bottom). Neuromasts are identified by GFP expression (green) and the tip of the notochord as a red line. Yellow arrow indicates shortest distance from tail tip to a neuromast. (b) Imaging analysis of the distance between the last neuromast and the tip of the tail (n = 3) under treatment with DMSO (negative control) or 11a (500 µM). P value calculated from t-test. (c) Study of zebrafish heart development under short treatment with 11a (500 µM) and dasatinib (10 µM). Compounds were added to 2 dpf zebrafish embryos and incubated for 4 h (n = 3). Subsequently, fresh media was added, and the fish imaged after 48 h incubation. |