1, 4??Dioxane??fused 4??anilinoquinazoline as inhibitors of epidermal growth factor receptor kinase

JY Lee, YK Park, SH Seo, IS So, HK Chung…

Index: Lee, Jae Yeol; Park, Yong Kyu; Seo, Seon Hee; So, In-Seop; Chung, Hee-Kyung; Yang, Beom-Seok; Lee, Sook Ja; Park, Hokoon; Lee, Yong Sup Archiv der Pharmazie, 2001 , vol. 334, # 11 p. 357 - 360

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Citation Number: 29

Abstract

Abstract The 4-anilinoquinazoline PD 153035 (1) is a potential antitumor agent which acts by inhibiting tyrosine kinase activity of epidermal growth factor receptor (EFGR) via competitive binding at the ATP site of enzyme. A series of cyclic analogues of PD 153035 bearing the 1, 4-dioxane ring was prepared by reaction of 6-chloro derivative 5 with several aniline nucleophiles. These were evaluated for their ability to inhibit the EGFR kinase and ...