151898-42-9Relevant articles and documents
Hybrid Quinazoline 1,3,5-Triazines as Epidermal Growth Factor Receptor (EGFR) Inhibitors with Anticancer Activity: Design, Synthesis, and Computational Study
Pathak, Prateek,Rimac, Hrvoje,Grishina, Maria,Verma, Amita,Potemkin, Vladimir
, p. 822 - 838 (2020/12/07)
We report a series of hybrid quinazoline-1,3,5-triazine derivatives as EGFR inhibitors, which were synthesised and tested by using a variety of in vitro, in silico, and in vivo techniques. The derivatives were found to be active against different cancer cell lines and nontoxic against normal ones, with compounds 7 c, 7 d, 7 e, and 7 j being the most potent ones. The derivatives were also evaluated for angiogenesis inhibition potency in chicken eggs, and molecular docking and dynamics simulation studies were carried out to elucidate the fundamental substituent groups essential for their bioactivity. Additionally, a SAR study of the derivatives was performed for future compound optimisation. These studies suggested that the derivatives have a high affinity towards EGFR with favourable pharmacological properties. The most active compound (7 e) was further evaluated for in vivo anticancer activity against DMBA-induced tumours in female Sprague-Dawley rats as well as its effects on plasma antioxidant status, biotransformation enzymes, and lipid profile. The study suggested that 7 e has lead properties against breast cancer and can serve as a starting compound for further development of anti-EGFR compounds.
Halogen-free expansion type flame retardant containing thiotriazinone phosphoramidate and preparation method thereof
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Paragraph 0052; 0053; 0054; 0055, (2016/10/31)
The invention relates to a halogen-free expansion type flame retardant containing thiotriazinone phosphoramidate and a preparation method thereof. Tricyanogen chloride, piperazine, organic amine, ammonia water and phosphoryl chloride serve as main raw materials, the compound is prepared through replacing and condensation reactions, and the advantages that the raw materials are easy to obtain and production is stable are achieved. The obtained compound containing P-N piperazine-riazine-phosphate ester structural units combines a carbon source, a gas source and an acid source into one molecular structure. The flame retardant has good water-resistant characteristic and can serve as flame retardant of most high-polymer materials, and good application prospects are achieved.
Inhibitors of histone deacetylase
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, (2008/06/13)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Inhibitors of histone deacetylase
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, (2008/06/13)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Inhibitors of histone deacetylase
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, (2008/06/13)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis
Hajduk, Philip J.,Dinges, Jürgen,Schkeryantz, Jeffrey M.,Janowick, David,Kaminski, Michele,Tufano, Michael,Augeri, David J.,Petros, Andrew,Nienaber, Vicki,Zhong, Ping,Hammond, Rachel,Coen, Michael,Beutel, Bruce,Katz, Leonard,Fesik, Stephen W.
, p. 3852 - 3859 (2007/10/03)
The Erm family of methyltransferases confers resistance to the macrolide-lincosamide-streptogramin type B (MLS) antibiotics through the methylation of 23S ribosomal RNA. Upon the methylation of RNA, the MLS antibiotics lose their ability to bind to the ribosome and exhibit their antibiotic activity. Using an NMR-based screen, we identified a series of triazinecontaining compounds that bind weakly to ErmAM. These initial lead compounds were optimized by the parallel synthesis of a large number of analogues, resulting in compounds which inhibit the Erm-mediated methylation of rRNA in the low micromolar range. NMR and X-ray structures of enzyme/inhibitor complexes reveal that the inhibitors bind to the S- adenosylmethionine binding site on the Erm protein. These compounds represent novel methyltransferase inhibitors that serve as new leads for the reversal of Erm-mediated MLS antibiotic resistance.