51704-66-6Relevant articles and documents
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic
Pace, Jennifer R.,Deberardinis, Albert M.,Sail, Vibhavari,Tacheva-Grigorova, Silvia K.,Chan, Kelly A.,Tran, Raymond,Raccuia, Daniel S.,Wechsler-Reya, Robert J.,Hadden, M. Kyle
supporting information, p. 3635 - 3649 (2016/05/24)
Itraconazole (ITZ) is an FDA-approved member of the triazole class of antifungal agents. Two recent drug repurposing screens identified ITZ as a promising anticancer chemotherapeutic that inhibits both the angiogenesis and hedgehog (Hh) signaling pathways. We have synthesized and evaluated first- and second-generation ITZ analogues for their anti-Hh and antiangiogenic activities to probe more fully the structural requirements for these anticancer properties. Our overall results suggest that the triazole functionality is required for ITZ-mediated inhibition of angiogenesis but that it is not essential for inhibition of Hh signaling. The synthesis and evaluation of stereochemically defined des-triazole ITZ analogues also provides key information as to the optimal configuration around the dioxolane ring of the ITZ scaffold. Finally, the results from our studies suggest that two distinct cellular mechanisms of action govern the anticancer properties of the ITZ scaffold.
Synthesis and properties of brassinosteroid biosynthesis inhibitor fluorescent probe with dansyl moiety
Hoshi, Tomoki,Yoshizawa, Yuko,Oh, Keimei
, p. 220 - 225 (2016/03/15)
Brassinosteroids (BRs) are important plant hormones that play key roles in plant development and defense responses to environmental cues. To explore the inhibition mechanism of BR biosynthesis, we report the synthesis of novel triazole derivatives with da
SMALL MOLECULE INHIBITORS OF FIBROSIS
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Paragraph 00333; 00336, (2015/01/06)
Described herein are compounds and compositions for the treatment of a fibrotic disease.