2507-80-4Relevant articles and documents
Hypervalent iodine in the synthesis of bridgehead heterocycles: A facile route to the synthesis of 6-arylimidazo[2,1-b]thiazoles using [hydroxy(tosyloxy)iodo]benzene
Aggarwal, Ranjana,Sumran, Garima
, p. 875 - 879 (2006)
α-Tosyloxyketones (2), readily accessible through hypervalent iodine oxidation of enolizable ketones (1) using [hydroxy(tosyloxy)iodo]benzene (HTIB) in acetonitrile, exclusively generates the 6-arylimidazo[2,1-b]thiazoles (4) on treatment with commerciall
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors
Abdel-Maksoud, Mohammed S.,Alach, Nour N.,Anbar, Hanan S.,El-Gamal, Mohammed I.,El-Gamal, Randa,Oh, Chang-Hyun,Sbenati, Rawan M.,Shehata, Mahmoud K.,Tarazi, Hamadeh,Zaraei, Seyed-Omar
, (2021/07/10)
This article reports on novel imidazothiazole derivatives as first-in-class potent and selective ErbB4 (HER4) inhibitors. There are no other reported selective inhibitors of this kinase in the literature, that's why they are considered as first-in-class. In addition, none of the reported non-selective ErbB4 inhibitors possesses imidazothiazole nucleus in its structure. Therefore, there is novelty in this work in both kinase selectivity and chemical structure. Compounds Ik and IIa are the most potent ErbB4 kinase inhibitor (IC50 = 15.24 and 17.70 nM, respectively). Compound Ik showed promising antiproliferative activity. It is selective towards cancer cell lines than normal cells. Its ability to penetrate T-47D cell membrane and inhibit ErbB4 kinase inside the cells has been confirmed. Moreover, both compound Ik and IIa have additional merits such as weak potency against hERG ion channels and against CYP 3A4 and 2D6. Molecular docking and dynamic simulation studies were carried out to explain binding interactions.
DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor
Liang, Dongdong,Li, Linhao,Lynch, Caitlin,Diethelm-Varela, Benjamin,Xia, Menghang,Xue, Fengtian,Wang, Hongbing
supporting information, p. 1039 - 1044 (2019/07/03)
The constitutive androstane receptor (CAR) is a xenobiotic sensor governing the transcription of genes involved in drug disposition, energy homeostasis, and cell proliferation. However, currently available human CAR (hCAR) agonists are nonselective, which