Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents

L Zhang, Q Zheng, Y Yang, H Zhou, X Gong…

Index: Zhang, Long; Zheng, Qingmei; Yang, Yingying; Zhou, Haojie; Gong, Xingjiang; Zhao, Shuyong; Fan, Chuanwen European Journal of Medicinal Chemistry, 2014 , vol. 82, p. 139 - 151

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Citation Number: 10

Abstract

Abstract A series of indolin-2-one analogues were designed and synthesized, and all of them exhibited excellent in vitro potency. The structure and in vivo activity or toxicity relationship (in-vivo SAR) investigation of indolin-2-one structural analogues was carried out. In vivo efficacy studies indicated that 3b significantly suppressed tumor growth in HT-29 and NCI-H460 xenografts without causing significant loss of body weight. Kinase assay ...