2475-82-3Relevant academic research and scientific papers
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor
Zhang, Hefeng,Peng, Xia,Dai, Yang,Shao, Jingwei,Ji, Yinchun,Sun, Yiming,Liu, Bo,Cheng, Xu,Ai, Jing,Duan, Wenhu
, p. 3956 - 3975 (2021/04/12)
The receptor tyrosine kinase Axl plays important roles in promoting cancer progression, metastasis, and drug resistance and has been identified as a promising target for anticancer therapeutics. We used molecular modeling-assisted structural optimization starting with the low micromolar potency compound 9 to discover compound 13c, a highly potent and orally bioavailable Axl inhibitor. Selectivity profiling showed that 13c could inhibit the well-known oncogenic kinase Met with equal potency to its inhibition of Axl superfamily kinases. Compound 13c significantly inhibited cellular Axl and Met signaling, suppressed Axl- and Met-driven cell proliferation, and restrained Gas6/Axl-mediated cancer cell migration or invasion. Furthermore, 13c exhibited significant antitumor efficacy in Axl-driven and Met-driven tumor xenograft models, causing tumor stasis or regression at well-tolerated doses. All these favorable data make 13c a promising therapeutic candidate for cancer treatment.
Containing 2 - methyl - 4 - [...] - 6 - yl of the chalcone analogs and its preparation and use
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Paragraph 0109; 0113; 0114, (2017/11/27)
The invention discloses a chalcone analogue containing 2-methyl-4-oxo-quinazoline-6-base, shown in a general formula (I), wherein the definitions of Ar1 and Ar2 are shown in the description. Besides, the invention further discloses a preparation method an
Organic field-effect transistors based on solution-processible dibenzotetrathiafulvalene derivatives
Yoshino, Takamasa,Shibata, Koji,Wada, Hiroshi,Bando, Yoshimasa,Ishikawa, Ken,Takezoe, Hideo,Mori, Takehiko
supporting information; experimental part, p. 200 - 201 (2010/03/02)
Organic field-effect transistors based on alkyl-substituted dibenzotetrathiafulvalenes (DBTTF) are fabricated by solution process. The molecules with butyl or longer alkyl groups are standing perpendicular to the substrates in the thin films, and the tran
Sulfonamides having antiangiogenic and anticancer activity
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, (2008/06/13)
Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating
Sulfonamides having antiangiogenic and anticancer activity
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, (2008/06/13)
Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
Sulfonamides having antiangiogenic and anticancer activity
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Page 22, (2008/06/13)
Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
1H-IMIDAZO[4,5-c]QUINOLINE DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES
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Page/Page column 67, (2008/06/13)
The invention relates to the use of imidazoquinolines and salts thereof in the treatment of protein kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, imidazoquinolines for use in the treatment of protein kinase dependent diseases, a method of treatment against said diseases, comprising administering the imidazoloquinolines to a warm-blooded animal, especially a human, pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease, novel imidazoquinolines, and a process for the preparation of the novel imidazoquinolines.
