N2,N4-BIS(4-(PIPERAZINE-1-YL)PHENYL)PIRIMIDINE-2,4-DIAMINE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor
作者:Brian J. Groendyke、Behnam Nabet、Mikaela L. Mohardt、Haisheng Zhang、Ke Peng、Eriko Koide、Calvin R. Coffey、Jianwei Che、David A. Scott、Adam J. Bass、Nathanael S. Gray
DOI:10.1021/acsmedchemlett.0c00338
日期:2021.1.14
Focal adhesion kinase (FAK) is a tyrosine kinase with prominent roles in protein scaffolding, migration, angiogenesis, and anchorage-independent cell survival and is an attractive target for the development of cancer therapeutics. However, current FAK inhibitors display dual kinase inhibition and/or significant activity on several kinases. Although multitargeted activity is at times therapeutically
HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM
申请人:Dams Géry Karel Julia
公开号:US20100280268A1
公开(公告)日:2010-11-04
The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the HIV gp41 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN36 (SEQ ID NO:1); a second helical polypeptide consisting essentially of the sequence of C34 (SEQ ID NO: 2) wherein said IQN36 is labeled with a light emitting fluorophore and said C34 is labeled with an ultra-violet excitable fluorophore.
该发明涉及一种基于荧光共振能量转移的高通量测试系统,用于测量HIV gp41六螺旋束的形成。在第一实施例中,当前发明涉及一种基于均匀时间分辨荧光的测试系统,包括基本上由IQN36序列(SEQ ID NO:1)组成的第一螺旋多肽;基本上由C34序列(SEQ ID NO:2)组成的第二螺旋多肽,其中所述的IQN36标记有发光荧光团,所述的C34标记有紫外激发荧光团。
N2,N4-bis(4-(piperazine-1-yl)phenyl)pirimidine-2,4-diamine derivative or pharmaceutically acceptable salt thereof, and composition containing same as active ingredient for preventing or treating cancer
申请人:KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
公开号:US09199944B2
公开(公告)日:2015-12-01
Disclosed herein are a new N2,N4-bis(4-(piperazin-1-yl)phenyl)pyrimidin-2,4-diamine derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition for the prevention or treatment of cancers containing the same as an active ingredient. The compound of the present invention has excellent inhibitory effects against the activities of anaplastic lymphoma kinase (ALK) and activated cdc42-associated kinase (ACK1) and thus can improve the therapeutic effects on the treatment of cancer cells having anaplastic lymphoma kinase fusion proteins such as EML4-ALK and NPM-ALK, and also effectively prevent the recurrence of cancers thus being useful as a pharmaceutical composition for the prevention and treatment of cancers.
Discovery of novel antitubercular drugs is an effective strategy against drug-resistant tuberculosis (TB). Our previous study has identified LPX-16j as a novel antitubercular compound. Herein, we perform a comprehensive structure–activity relationship (SAR) based on LPX-16j, indicating that the central pyrimidine ring moiety was crucial for the antitubercular activities of its derivatives, and replacing
Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment
作者:Chi Hoon Park、Hyeonjeong Choe、In-Young Jang、So Yeong Kwon、Muhammad Latif、Heung Kyoung Lee、Hyeon Ji Lee、Eun Hye Yang、Jeong In Yun、Chong Hak Chae、Sung Yun Cho、Sang Un Choi、Jae Du Ha、Heejung Jung、Hyoung Rae Kim、Pilho Kim、Chong Ock Lee、Chang-Soo Yun、Kwangho Lee
DOI:10.1016/j.bmcl.2013.08.090
日期:2013.11
The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstrates in vivo efficacy comparable to Crizotinib in xenograft mice model. (c) 2013 Elsevier Ltd. All rights reserved.