1343447-99-3Relevant academic research and scientific papers
Design, synthesis and in vitro evaluation of benzothiazole-based ureas as potential ABAD/17β-HSD10 modulators for Alzheimer's disease treatment
Hroch, Lukas,Benek, Ondrej,Guest, Patrick,Aitken, Laura,Soukup, Ondrej,Janockova, Jana,Musil, Karel,Dohnal, Vlastimil,Dolezal, Rafael,Kuca, Kamil,Smith, Terry K,Gunn-Moore, Frank,Musilek, Kamil
supporting information, p. 3675 - 3678 (2016/07/21)
Amyloid-beta peptide (Aβ) has been recognized to interact with numerous proteins, which may lead to pathological changes in cell metabolism of Alzheimer's disease (AD) patients. One such known metabolic enzyme is mitochondrial amyloid-binding alcohol dehydrogenase (ABAD), also known as 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10). Altered enzyme function caused by the Aβ-ABAD interaction, was previously shown to cause mitochondrial distress and a consequent cytotoxic effect, therefore providing a feasible target in AD drug development. Based on previous frentizole derivatives studies, we report two novel series of benzothiazolyl ureas along with novel insights into the structure and activity relationships for inhibition of ABAD. Two compounds (37, 39) were identified as potent ABAD inhibitors, where compound 39 exhibited comparable cytotoxicity with the frentizole standard; however, one-fold higher cytotoxicity than the parent riluzole standard. The calculated and experimental physical chemical properties of the most potent compounds showed promising features for blood–brain barrier penetration.
Synthesis of benzothiazole derivatives and their biological evaluation as anticancer agents
Caputo, Rosanna,Calabro, Maria Luisa,Micale, Nicola,Schimmer, Aaron D.,Ali, Moshin,Zappala, Maria,Grasso, Silvana
, p. 2644 - 2651 (2012/11/07)
This article describes the synthesis and the biological evaluation of two sets of benzothiazole derivatives bearing at C-2 an arylamide (1a-e, 2a-e) or an arylurea (3a-d, 4a-d) moiety. Five compounds (3d and 4a-d) were selected and screened by the National Cancer Institute for the in vitro primary anticancer assay against a panel of 60 human tumor cell lines. Compounds 4a and 4c showed interesting anticancer activities, more marked for compound 4c. All compounds were also submitted to a preliminary in vitro assay as potential inhibitors of the ubiquitin-activating enzyme (E1), but they lacked significant activity. Springer Science+Business Media, LLC 2011.
