a-419259 and Neoplasms

a-419259 has been researched along with Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for a-419259 and Neoplasms

Article	Year
Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors. Bioorganic & medicinal chemistry letters, 2013, May-15, Volume: 23, Issue:10 The synthesis and biological evaluation of novel Tie-2 kinase inhibitors are presented. Based on the pyrrolopyrimidine chemotype, several new series are described, including the benzimidazole series by linking a benzimidazole to the C5-position of the 4-amino-pyrrolopyrimidine core and the ketophenyl series synthesized by incorporating a ketophenyl group to the C5-position. Medicinal chemistry efforts led to potent Tie-2 inhibitors. Compound 15, a ketophenyl pyrrolopyrimidine urea analog with improved physicochemical properties, demonstrated favorable in vitro attributes as well as dose responsive and robust oral tumor growth inhibition in animal models. Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Humans; Male; Molecular Structure; Neoplasms; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Rats; Rats, Sprague-Dawley; Receptor, TIE-2; Structure-Activity Relationship; Xenograft Model Antitumor Assays	2013

Article

Year

Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors.

Bioorganic & medicinal chemistry letters, 2013, May-15, Volume: 23, Issue:10

The synthesis and biological evaluation of novel Tie-2 kinase inhibitors are presented. Based on the pyrrolopyrimidine chemotype, several new series are described, including the benzimidazole series by linking a benzimidazole to the C5-position of the 4-amino-pyrrolopyrimidine core and the ketophenyl series synthesized by incorporating a ketophenyl group to the C5-position. Medicinal chemistry efforts led to potent Tie-2 inhibitors. Compound 15, a ketophenyl pyrrolopyrimidine urea analog with improved physicochemical properties, demonstrated favorable in vitro attributes as well as dose responsive and robust oral tumor growth inhibition in animal models.

Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Humans; Male; Molecular Structure; Neoplasms; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Rats; Rats, Sprague-Dawley; Receptor, TIE-2; Structure-Activity Relationship; Xenograft Model Antitumor Assays

2013