39217-02-2Relevant academic research and scientific papers
STK19 INHIBITORS FOR TREATMENT OF CANCER
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Paragraph 00413-00415; 00417-00418, (2020/07/14)
Provided herein are compositions and methods for the treatment and prevention of cancer, including melanoma.
Quinazoline derivatives, composition and application thereof
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Paragraph 0096; 0097, (2018/07/06)
The invention relates to quinazoline derivatives as shown in a formula I as described in the specification, a composition and application thereof as a PGK1 inhibitor for preparing anti-tumor drugs andapplication thereof in treating malignant tumors.
Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo
Wang, Xiao-Meng,Xin, Min-Hang,Xu, Jing,Kang, Bo-Rui,Li, Yan,Lu, She-Min,Zhang, San-Qi
, p. 382 - 395 (2015/05/05)
In the present study, a series of m-(4-morpholinoquinazolin-2-yl)benzamides were designed, synthesized and characterized. The antiproliferative activities of the synthesized compounds were evaluated against two human cell lines (HCT-116 and MCF-7). Compounds with IC50 values below 4 μM were further evaluated against U-87 MG and A549 cell lines. Among these evaluated compounds, compound T10 displayed a remarkable antiproliferative effect in vitro. The hoechst staining assay showed that compound T10 caused morphological changes. The cell cycle and apoptosis assay further indicated that compound T10 can arrest HCT-116 cells in G2/M and G0/G1 phase and induce apoptosis. PI3K enzyme assays indicated that compounds T7 and T10 selectively inhibit PI3K±. A Western bolt assay further suggested that compound T10 can block the PI3K/Akt/mTOR pathway. Moreover, compound T10 inhibited tumor growth on a mice S180 homograft model. These findings directly identify m-(4-morpholinoquinazolin-2-yl)benzamide derivatives as novel anticancer agents.
Molecular features of the prazosin molecule required for activation of Transport-P
da Silva, Joaquim Fernando Mendes,Walters, Marcus,Al-Damluji, Saad,Ganellin, C. Robin
, p. 7254 - 7263 (2008/12/23)
Closely related structural analogues of prazosin have been synthesised and tested for inhibition and activation of Transport-P in order to identify the structural features of the prazosin molecule that appear to be necessary for activation of Transport-P. So far, all the compounds tested are less active than prazosin. It is shown that the structure of prazosin appears to be very specific for the activation. Only quinazolines have been found to activate, and the presence of the 6,7-dimethoxy and 4-amino groups appears to be critically important.
Discovery of potent CCR4 antagonists: Synthesis and structure-activity relationship study of 2,4-diaminoquinazolines
Yokoyama, Kazuhiro,Ishikawa, Noriko,Igarashi, Susumu,Kawano, Noriyuki,Hattori, Kazuyuki,Miyazaki, Takahiro,Ogino, Shin-ichi,Matsumoto, Yuzo,Takeuchi, Makoto,Ohta, Mitsuaki
, p. 7021 - 7032 (2008/12/22)
A new series of quinazolines that function as CCR4 antagonists were discovered during the screening of our corporate compound libraries. Subsequent compound optimization elucidated the structure-activity relationships and led the identification of 2-(1,4′-bipiperidine-1′-yl)-N-cycloheptyl-6,7-dimethoxyquinazolin-4-amine 14a, which showed potent inhibition in the [35S]GTPγS-binding assay (IC50 = 18 nM). This compound also inhibited the chemotaxis of human and mouse CCR4-expressing cells (IC50 = 140 nM, 39 nM).
