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
Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives
Salado, Irene G.,Baán, Adrienn,Verdeyen, Tomas,Matheeussen, An,Caljon, Guy,Van der Veken, Pieter,Kiekens, Filip,Maes, Louis,Augustyns, Koen
, p. 18 - 26 (2018/04/02)
Human African trypanosomiasis is causing thousands of deaths every year in the rural areas of sub-saharan Africa. There is a high unmet medical need since the approved drugs are poorly efficacious, show considerable toxicity and are not easy to administer
