19430-24-1Relevant articles and documents
Enantioselective Strecker and Allylation Reactions with Aldimines Catalyzed by Chiral Oxazaborolidinium Ions
Kang, Ki-Tae,Park, Sang Hyun,Ryu, Do Hyun
supporting information, p. 6679 - 6683 (2019/09/12)
Chiral oxazaborolidinium ion (COBI)-catalyzed enantioselective nucleophilic addition reactions of aldimines using tributyltin cyanide and allyltributylstannane have been developed. Various α-aminonitriles and homoallylic amines were synthesized in high yi
Design, Synthesis, and Biological Activity of New N -(Phenylmethyl)-benzoxazol-2-thiones as Macrophage Migration Inhibitory Factor (MIF) Antagonists: Efficacies in Experimental Pulmonary Hypertension
Le Hiress, Morane,Akagah, Bernardin,Bernadat, Guillaume,Tu, Ly,Thuillet, Rapha?l,Huertas, Alice,Phan, Carole,Fadel, Elie,Simonneau, Gérald,Humbert, Marc,Jalce, Ga?l,Guignabert, Christophe
, p. 2725 - 2736 (2018/04/23)
Macrophage migration inhibitory factor (MIF) is a key pleiotropic mediator and a promising therapeutic target in cancer as well as in several inflammatory and cardiovascular diseases including pulmonary arterial hypertension (PAH). Here, a novel series of N-(phenylmethyl)-benzoxazol-2-thiones 5-32 designed to target the MIF tautomerase active site was synthesized and evaluated for its effects on cell survival. Investigation of structure-activity relationship (SAR) particularly at the 5-position of the benzoxazole core led to the identification of 31 that potently inhibits cell survival in DU-145 prostate cancer cells and pulmonary endothelial cells derived from patients with idiopathic PAH (iPAH-ECs), two cell lines for which survival is MIF-dependent. Molecular docking studies helped to interpret initial SAR related to MIF tautomerase inhibition and propose preferred binding mode for 31 within the MIF tautomerase active site. Interestingly, daily treatment with 31 started 2 weeks after a subcutaneous monocrotaline injection regressed established pulmonary hypertension in rats.
Aryl schiff base derivate and preparation method and application thereof
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Paragraph 0026; 0027; 0028; 0029; 0030; 0031-0038, (2017/08/28)
The invention discloses an aryl schiff base derivate and preparation method and a preparation method and application thereof. The structural formula of the aryl schiff base derivate sees description. The preparation method is characterized in that a certa