- Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline as potential EGFR inhibitors
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Eight series of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline were designed, synthesized and evaluated for the IC50 values against three cancer cell lines (A549, MCF-7 and PC-3). Most of the forty nine target compounds showed excellent antiproliferative activity against one or several cancer cell lines. The compound 13a showed the best activity against A549, MCF-7 and PC-3 cancer cell lines, with the IC50 values of 1.09 ± 0.04 μM, 1.34 ± 0.13 μM and 1.23 ± 0.09 μM, respectively. Eight selected compounds were further selected to evaluated for the inhibitory activity against EGFR kinase. Three of them showed equal activity against EGFR kinase to positive control afatinib. AnnexinV-FITC, propidium iodide (PI) double staining and acridine orange single staining results indicated that the compound 13a could induce apoptosis of human lung cancer A549 cells.
- OuYang, Yiqiang,Zou, Wensheng,Peng, Liang,Yang, Zunhua,Tang, Qidong,Chen, Mengzi,Jia, Shuang,Zhang, Hong,Lan, Zhou,Zheng, Pengwu,Zhu, Wufu
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- MULTISUBSTITUTED AROMATIC COMPOUNDS AS INHIBITORS OF THROMBIN
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There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.
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Paragraph 0299-0300
(2017/12/07)
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- TYK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
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Paragraph 00472; 00474
(2015/09/28)
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- Expeditious one-pot synthesis of C3-piperazinyl-substituted quinolines: Key precursors to potent c-Met inhibitors
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An effective one-pot synthesis of quinolines bearing diverse C3-piperazinyl functions was developed by using a modified Friedlaender's protocol. The method not only enables the synthesis of our early reported c-Met inhibitor on a large scale, but also provides a way to generate novel multi-substituted quinolines for further structure-activity relationship (SAR) study.
- Wang, Yuanxiang,Ai, Jing,Liu, Gang,Geng, Meiyu,Zhang, Ao
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supporting information; scheme or table
p. 5930 - 5933
(2011/10/08)
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- MULTISUBSTITUTED AROMATIC COMPOUNDS AS INHIBITORS OF THROMBIN
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There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.
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Page/Page column 79
(2011/10/31)
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- Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles
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We have previously reported the discovery and initial SAR of the [1,7]naphthyridine-3-carbonitriles and quinoline-3-carbonitriles as Tumor Progression Loci-2 (Tpl2) kinase inhibitors. In this paper, we report new SAR efforts which have led to the identifi
- Kaila, Neelu,Green, Neal,Li, Huan-Qiu,Hu, Yonghan,Janz, Kristin,Gavrin, Lori Krim,Thomason, Jennifer,Tam, Steve,Powell, Dennis,Cuozzo, John,Hall, J. Perry,Telliez, Jean-Baptiste,Hsu, Sang,Nickerson-Nutter, Cheryl,Wang, Qin,Lin, Lih-Ling
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p. 6425 - 6442
(2008/04/05)
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