116133-09-6Relevant articles and documents
Di- and tri-substituted s-triazine derivatives: Synthesis, characterization, anticancer activity in human breast-cancer cell lines, and developmental toxicity in zebrafish embryos
El-Faham, Ayman,Farooq, Muhammad,Almarhoon, Zainab,Alhameed, Rakia Abd,Wadaan, Mohammad A.M.,de la Torre, Beatriz G.,Albericio, Fernando
, (2020)
Here we report on a small library based on a 4-aminobenzonitile-s-triazine moiety. We used a straightforward orthogonal synthetic pathway to prepare di- and tri-substituted s-triazine derivatives, whose basic structure was modified. The newly synthesized compounds were fully characterized by 1H NMR, 13C NMR and elemental analysis. They showed strong anticancer activity against two human breast cancer cell lines (MIDA-MB-231 and MCF-7), with IC50 values less than 1 μM. These s-triazine compounds were generally more selective towards hormone receptor-positive breast cancer cell line MCF-7 than the triple negative MDA-MB-231 cell line. Zebrafish embryos were used to test the developmental toxicity of the target compounds in vivo. The phenotype of embryos treated with the derivatives resembled that of those treated with estrogen disruptors. This observation strongly supports the notion that that these compounds induce their anticancer activity in human breast cancer cells via targeting the estrogen and progesterone receptors.
Indoloxytriazines as binding molecules for the JAK2 JH2 pseudokinase domain and its V617F variant
Newton, Ana S.,Liosi, Maria-Elena,Henry, Sean P.,Deiana, Luca,Faver, John C.,Krimmer, Stefan G.,Puleo, David E.,Schlessinger, Joseph,Jorgensen, William L.
supporting information, (2021/07/20)
Small molecules that selectively bind to the pseudokinase JH2 domain over the JH1 kinase domain of JAK2 kinase are sought. Virtual screening led to the purchase of 17 compounds among which 9 were found to bind to V617F JAK2 JH2 with affinities of 40 – 300
Heterocyclic compounds as well as preparation method and application thereof
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Paragraph 0221; 0222; 0223; 0264; 0265, (2018/07/30)
The invention belongs to the field of medicines and particularly relates to heterocyclic compounds with the structural characteristics shown in formula (I) or pharmaceutically acceptable salts, a preparation method and an application of the heterocyclic compounds as a nucleotide oxidative damage repairase MTH1 inhibitor. Pharmacological experiment results indicate that the compounds have significant inhabitation effects on the activity of MTH1 and can be used for preventing and treating clinical diseases related to MTH1.
