KDR inhibitor with the intramolecular non-bonded interaction: Conformation–activity relationships of novel indole-3-carboxamide derivatives

T Honda, H Nagahara, H Mogi, M Ban…

Index: Honda, Takahiro; Nagahara, Hironori; Mogi, Hiroyuki; Ban, Masakazu; Aono, Hiroyuki Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 6 p. 1782 - 1785

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Citation Number: 3

Abstract

We previously reported that compound 1, having a similar conformation to PTK787 (2) by forming a pseudo ring structure with an intramolecular non-bonded S–O interaction, exhibited a potent inhibitory activity against VEGFR2 tyrosine kinase (KDR). 1 Applying the ideas of pseudo ring formations, we have designed three types of novel indole carboxamide derivatives 5–7 with an intramolecular hydrogen bonding or non-bonded S–O interaction. ...