1709-59-7Relevant articles and documents
Pyrrole and pyrazole compound of preparation and use as medicaments (by machine translation)
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Paragraph 0091; 0092; 0093; 0094, (2018/03/26)
The invention relates to the field of medical technology, this invention has offered a kind of sulfonamide and nitrogen mixed uncle butane pyrrole and pyrazole compound, including optical isomers, racemic modification, and any combination of the trans isomer or a pharmaceutically acceptable salt thereof, having a structure of formula (I); the invention also provides the preparation method of the compound and its application, in particular in the preparation of anti-tumor drug application. (by machine translation)
Novel 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors
Barbosa, Maria Letícia De Castro,Lima, Lídia Moreira,Tesch, Roberta,Sant'Anna, Carlos Mauricio R.,Totzke, Frank,Kubbutat, Michael H.G.,Sch?chtele, Christoph,Laufer, Stefan A.,Barreiro, Eliezer J.
, p. 1 - 14 (2013/12/04)
Novel 2-chloro-4-anilino-quinazolines designed as EGFR and VEGFR-2 dual inhibitors were synthesized and evaluated for inhibitory effects. EGFR and VEGFR-2 are validated targets in cancer therapy and combined inhibition might be synergistic for both antitumor activity and resistance prevention. The biological data obtained proved the potential of 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors, highlighting compound 8o, which was approximately 7-fold more potent on VEGFR-2 and approximately 11-fold more potent on EGFR compared to the prototype 7. SAR and docking studies allowed the identification of pharmacophoric groups for both kinases and demonstrated the importance of a hydrogen bond donor at the para position of the aniline moiety for interaction with conserved Glu and Asp amino acids in EGFR and VEGFR-2 binding sites.
PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS
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Page/Page column 101-102, (2011/02/24)
The present invention relates to compounds II useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the invention.