230955-55-2Relevant academic research and scientific papers
HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and in Vitro and in Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability
Elwaie, Tamer A.,Abbas, Safinaz E.,Aly, Enayat I.,George, Riham F.,Ali, Hamdy,Kraiouchkine, Nikolai,Abdelwahed, Khaldoun S.,Fandy, Tamer E.,El Sayed, Khalid A.,Abd Elmageed, Zakaria Y.,Ali, Hamed I.
, p. 15906 - 15945 (2021/01/09)
HER2 kinase as a well-established target for breast cancer (BC) therapy is associated with aggressive clinical outcomes; thus, herein we present structural optimization for HER2-selective targeting. HER2 profiling of the developed derivatives demonstrated
Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines
Li, Ri-Dong,Zhang, Xin,Li, Qiao-Yan,Ge, Ze-Mei,Li, Run-Tao
supporting information; experimental part, p. 3637 - 3640 (2011/08/06)
On the basis of combination strategy, a novel series of EGFR inhibitors were designed and synthesized by combination of dithiocarbamic acid esters and 4-anilinoquinazolines. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay in three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Two compounds (11d and 11f) were found more potent against all three cell lines and five compounds (11a, 11d-11g) were found more potent against both MDA-MB-468 and SK-BR-3 than Lapatinib. SAR studies revealed that the substituents on C6 and C7 positions of quinazoline, the amine component of dithiocarbamate moiety and the linker greatly affected the activity. This work provides a promising new strategy for the preparation of potent tyrosine kinase inhibitors.
QUINAZOLINE DERIVATIVES,PREPARATION METHODS AND USES THEREOF
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Page/Page column 14, (2008/12/08)
The present invention has disclosed a compound of formula I and a pharmaceutically acceptable salt or a solvate thereof, wherein the substituents are as defined in the description. The invention has also disclosed a method for preparing the compound of formula I, the pharmaceutical compositions comprising the same and their uses in the preparation of an anti- tumor medicament.
Quinazoline Derivatives, Preparation Methods and Uses Thereof
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Page/Page column 8-9, (2009/01/20)
The present invention has disclosed a compound of formula I and a pharmaceutically acceptable salt or a solvate thereof, wherein the substituents are as defined in the description. The invention has also disclosed a method for preparing the compound of formula I, the pharmaceutical compositions comprising the same and their uses in the preparation of an anti-tumor medicament.
MULTI-FUNCTIONAL SMALL MOLECULES AS ANTI-PROLIFERATIVE AGENTS
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Page/Page column 173, (2008/06/13)
The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors
Zhang, Yue-Mei,Cockerill, Stuart,Guntrip, Stephen B.,Rusnak, David,Smith, Kathryn,Vanderwall, Dana,Wood, Edgar,Lackey, Karen
, p. 111 - 114 (2007/10/03)
A series of 6-alkoxy-4-anilinoquinazoline compounds was prepared and evaluated for in vitro inhibition of the erbB2 and EGFR kinase activity. The IC50 values of the best compounds were below 0.10 uM. Further, several of these compounds inhibit the growth of erbB2 and EGFR over-expressing tumor cell lines at concentrations below 1 uM.
