sr-3029 and Neoplasms

sr-3029 has been researched along with Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for sr-3029 and Neoplasms

Article	Year
Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorganic & medicinal chemistry letters, 2013, Aug-01, Volume: 23, Issue:15 The development of a series of potent and highly selective casein kinase 1δ/ε (CK1δ/ε) inhibitors is described. Starting from a purine scaffold inhibitor (SR-653234) identified by high throughput screening, we developed a series of potent and highly kinase selective inhibitors, including SR-2890 and SR-3029, which have IC₅₀ ≤ 50 nM versus CK1δ. The two lead compounds have ≤100 nM EC50 values in MTT assays against the human A375 melanoma cell line and have physical, in vitro and in vivo PK properties suitable for use in proof of principle animal xenograft studies against human cancer cell lines. Topics: Animals; Antineoplastic Agents; Binding Sites; Casein Kinase 1 epsilon; Casein Kinase Idelta; Catalytic Domain; Cell Line, Tumor; Cell Survival; Half-Life; Humans; Mice; Microsomes, Liver; Molecular Docking Simulation; Neoplasms; Purines; Rats; Structure-Activity Relationship; Transplantation, Heterologous	2013

Article

Year

Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties.

Bioorganic & medicinal chemistry letters, 2013, Aug-01, Volume: 23, Issue:15

The development of a series of potent and highly selective casein kinase 1δ/ε (CK1δ/ε) inhibitors is described. Starting from a purine scaffold inhibitor (SR-653234) identified by high throughput screening, we developed a series of potent and highly kinase selective inhibitors, including SR-2890 and SR-3029, which have IC₅₀ ≤ 50 nM versus CK1δ. The two lead compounds have ≤100 nM EC50 values in MTT assays against the human A375 melanoma cell line and have physical, in vitro and in vivo PK properties suitable for use in proof of principle animal xenograft studies against human cancer cell lines.

Topics: Animals; Antineoplastic Agents; Binding Sites; Casein Kinase 1 epsilon; Casein Kinase Idelta; Catalytic Domain; Cell Line, Tumor; Cell Survival; Half-Life; Humans; Mice; Microsomes, Liver; Molecular Docking Simulation; Neoplasms; Purines; Rats; Structure-Activity Relationship; Transplantation, Heterologous

2013