Sudta, Pichit; Kirk, Nicholas; Bezos, Anna; Gurlica, Anthony; Mitchell, Rhys; Weber, Thomas; Willis, Anthony C.; Prabpai, Samran; Kongsaeree, Palangpon; Parish, Christopher R.; Suksamrarn, Sunit; Kelso, Michael J. published the artcile< Synthesis, Structural Characterisation, and Preliminary Evaluation of Non-Indolin-2-one-based Angiogenesis Inhibitors Related to Sunitinib (Sutent)>, Electric Literature of 30095-98-8, the main research area is sunitinib analog preparation angiogenesis inhibitor SAR.
The indolin-2-one fused-ring system and the 2,4-dimethylpyrrole unit represent key structural motifs in the anticancer drug sunitinib (Sutent) and predecessor angiogenesis inhibitors that have undergone anticancer clin. trials (e.g. semaxanib, SU5416). In pursuit of novel anti-angiogenic scaffolds, we were interested in identifying whether the indolin-2-one group in these structures could be modified without losing activity. This paper describes novel condensation chem. used to prepare a test series of (E)- and (Z)-alkenes related to SU5416 that retain the 2,4-dimethylpyrrole unit while incorporating ring-opened indolin-2-ones. Unique structural characteristics were identified in the compounds, such as intramol. hydrogen bonds in the (Z)-alkenes, and several examples were shown to possess significant anti-angiogenic activity in a rat aorta in vitro model of angiogenesis. The work demonstrates that the indolin-2-one moiety is not an absolute requirement for angiogenesis inhibition in the sunitinib/SU5416 class.
Australian Journal of Chemistry published new progress about Antiangiogenic agents. 30095-98-8 belongs to class esters-buliding-blocks, and the molecular formula is C9H9NO4, Electric Literature of 30095-98-8.
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