79537-70-5Relevant articles and documents
Synthesis of Thiourea and Sulfonylurea Derivatives of Chalcones and Flavones and their Biological Evaluation
Pratap, Ram,Satyanarayana, Mavurapu,Shukla, Poonam,Srivastava, Arvind K,Tiwari, Priti,Tripathi, Brajendra K
, p. 341 - 345 (2021/11/22)
Chalcone and flavone derivatives based on thiourea and sulfonylurea (6, 7a and 7b, 13a and 13b) were synthesized and confirmed by spectral data. All the target compounds were evaluated for in vivo antihyperglycemic activity in sucrose loaded model (SLM) a
Contra-thermodynamic E → Z isomerization of cinnamamides via selective energy transfer catalysis
Becker, Marc R.,Morack, Tobias,Robertson, Jack,Metternich, Jan B.,Mück-Lichtenfeld, Christian,Daniliuc, Constantin,Burley, Glenn A.,Gilmour, Ryan
supporting information, (2020/05/25)
A bio-inspired, photocatalytic E → Z isomerization of cinnamides is reported using inexpensive (?)-riboflavin (vitamin B2) under irradiation at λ = 402 nm. This operationally simple transformation is compatible with a range of amide derivatives including –NR2, –NHSO2R and N(Boc)2 (up to 99:1 Z:E). Selective energy transfer from the excited state photocatalyst to the starting E-isomer ensures that directionality is achieved: The analogous process with the Z-isomer is inefficient due to developing allylic strain causing chromophore deconjugation. This is supported by X-ray analysis and Stern-Volmer photo-quenching studies. Preliminary validation of the method in manipulating the conformation of a simple model Leu-enkephalin penta-peptide is disclosed via the incorporation of a cinnamamide-based amino acid.
T790M mutant EGFR inhibitors and its application in the preparation of antineoplastic
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Paragraph 0090; 0092; 0094; 0095, (2018/03/25)
The invention provides a T790M mutant EGFR inhibitor and an application of the same in preparation of antitumor drugs. The inhibitor is a pyrimidine compound with structural characteristics of a formula (I). The compound can inhibit various tumor cells and particularly can act on EGFR L858R/T790M and EGFR E 745_A750/T790M lung cancer cells selectively, and the IC 50 of the compound is 10 timers and even 100 times higher than that of wild cancer cells. The compound is the protease inhibitor which is capable of overcoming prior EGFR-TKI drug resistance and has selectivity and can be applied to preparation of antitumor drugs. (img file= 'DDAS0000708455660000011. TIF' wi= '716' he= '576'/).