Please use this identifier to cite or link to this item: https://ir.swu.ac.th/jspui/handle/123456789/14013
ชื่อเรื่อง: Synthesis, structural characterisation, and preliminary evaluation of non-indolin-2-one-based angiogenesis inhibitors related to sunitinib (Sutent®)
ผู้แต่ง: Sudta P.
Kirk N.
Bezos A.
Gurlica A.
Mitchell R.
Weber T.
Willis A.C.
Prabpai S.
Kongsaeree P.
Parish C.R.
Suksamrarn S.
Kelso M.J.
Keywords: Angiogenesis inhibitors
Anti-angiogenic activity
Anticancer drug
Fused-ring system
In-vitro models
Intra-molecular hydrogen bonds
Structural characteristics
Structural motifs
Scaffolds
Hydrocarbons
วันที่เผยแพร่: 2013
บทคัดย่อ: 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 clinical 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 chemistry 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 intramolecular 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. © 2013 CSIRO.
URI: https://ir.swu.ac.th/jspui/handle/123456789/14013
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84882683064&doi=10.1071%2fCH13219&partnerID=40&md5=b6872cd822d2d762810d0cc43aedc99e
ISSN: 49425
Appears in Collections:Scopus 1983-2021

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