Ontology highlight
ABSTRACT:
SUBMITTER: Wu J
PROVIDER: S-EPMC4027470 | biostudies-literature | 2013 Oct
REPOSITORIES: biostudies-literature
Wu Jianwei J Chen Wenteng W Xia Guangxin G Zhang Jing J Shao Jiaan J Tan Biqin B Zhang Chunchun C Yu Wanwan W Weng Qinjie Q Liu Haiyan H Hu Miao M Deng Hailin H Hao Yu Y Shen Jingkang J Yu Yongping Y
ACS medicinal chemistry letters 20130806 10
This letter describes the construction of conformationally constrained quinazoline analogues. Structure-activity relationship studies led to the identification of the lead compound 9n . Compound 9n exhibits effective in vitro activity against A431(WT,overexpression) and H1975([L858R/T790M]) cancer cell lines but is significantly less effective against EGFR negative cancer cell lines (SW620, A549, and K562). Compound 9n was also assessed for potency in enzymatic assays and in vivo antitumor studi ...[more]