91506-71-7Relevant academic research and scientific papers
Tumor-Activated Benzothiazole Inhibitors of Stearoyl-CoA Desaturase
Williams, Noelle S.,Gonzales, Stephen,Naidoo, Jacinth,Rivera-Cancel, Giomar,Voruganti, Sukesh,Mallipeddi, Prema,Theodoropoulos, Panayotis C.,Geboers, Sophie,Chen, Hong,Ortiz, Francisco,Posner, Bruce,Nijhawan, Deepak,Ready, Joseph M.
, p. 9773 - 9786 (2020/10/19)
A series of N-acyl benzothiazoles shows selective and potent cytotoxicity against cancer cell lines expressing cytochrome P450 4F11. A prodrug form is metabolized by cancer cells into an active inhibitor of stearoyl-CoA desaturase (SCD). Substantial variation on the acyl portion of the inhibitors allowed the identification of (R)-27, which balanced potency, solubility, and lipophilicity to allow proof-of-concept studies in mice. The prodrugs were activated inside the tumor, where they can arrest tumor growth. Together, these observations offer promise that a tumor-activated prodrug strategy might exploit the essentiality of SCD for tumor growth, while avoiding toxicity associated with systemic SCD inhibition.
METHODS AND COMPOSITIONS FOR SELECTIVE AND TARGETED CANCER THERAPY
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Page/Page column 169; 170, (2015/03/28)
Provided herein are methods and compositions for selective and targeted cancer therapy, in particular certain benzothiophenes, benzothiazoles, oxalamides, N-acyl ureas and chromones, and their use in selectively treating certain adenocarcinomas. In some embodiments, the selective toxicity of the compounds may be mediated through SCD1 and/or CYP450 such as CYP4F11.
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.
Synthesis, Photolysis and Pyrolysis of 1-(2'-Benzothiazolyl)-5-aryltetrazoles
Kamala, K.,Rao, P. Jayaprasad,Reddy, K. Kondal
, p. 1194 - 1196 (2007/10/02)
Aroylaminobenzothiazoles (II), have been converted into 1-(2'-benzothiazolyl)-5-aryltetrazoles (IV) by treatment with PCl5 followed by azidolysis with sodium azide in aequeous acetone solution.Pyrolysis of IV in tetralin affords exclusively 2-aryl-s-triaz
