57427-78-8Relevant articles and documents
Design and development of 5-(4H)-oxazolones as potential inhibitors of human carbonic anhydrase VA: towards therapeutic management of diabetes and obesity
Alajmi, Mohamed F.,Das Mahapatra, Amarjyoti,Datta, Bhaskar,Hassan, Md. Imtaiyaz,Hussain, Afzal,Khan, Parvez,Queen, Aarfa,Rehman, Md. Tabish,Yousuf, Mohd
, (2020)
Inhibitors of carbonic anhydrase (CAIs) hold promise for addressing various diseases, including cancer, diabetes, and other metabolic syndromes. CAV is the only isoform present in the mitochondria and is considered a potential drug target for obesity. In
Synthesis and luminescence properties of analogues of the green fluorescent protein chromophore
Esteves, Cátia I. C.,Guieu, Samuel,Rocha, Jo?o,Silva, Artur M. S.,da Silva Fonseca, Inês
, (2020/02/18)
The green fluorescent protein (GFP) is extensively used as a biomarker for fluorescence biological imaging. The chromophore in GFP is only fluorescent when confined into the β–barrel of the protein. Similarly, synthetic analogues of the fluorophore of GFP
Synthesis and cytotoxicity of novel dispiro derivatives of 5-arylidenoxazolones, potential inhibitors of p53—MDM2 protein-protein interaction
Beloglazkina,Skvortsov,Tafeenko,Majouga,Zyk,Beloglazkina
, p. 562 - 569 (2018/07/06)
Regioselective synthesis of new dispiro indolinones combining both an indolinone and an oxazolone fragment in their structure comprised the 1,3-dipolar cycloaddition of azomethine ylides, generated in situ from isatin and sarcosine, at 2-aryl-5-arylmethylidene-substituted 1,3-oxazol-5(4H)-ones. When ortho and para halogen atoms were present in the aromatic substituents of the starting oxazolones, complex mixtures containing large amounts of oxazoline ring opening products and their dispiro derivatives were formed. The cytotoxicity of compounds was tested by MTT on LNCaP, PC3, HCT116, MCF7, A549, HEK, and VA13 cell lines. The compound possessing the best cytotoxicity revealed the IC50 = 1.08±0.96 μM towards the p53- expressing LNCaP cells and lower activity (IC50 = 3.21±1.45 μM) towards the non-expressing p53 protein PC3 cells, however, it has proved inactive towards the HCT cells, both expressing (HCТ+/+) and non-expressing (HCT–/–) p53.