Article
Synthesis and cytotoxicity of Baylis-Hillman template derived betulinic acid-triazole conjugates
Tetrahedron
(2016)
Abstract
Several alkynes and azides were prepared starting from betulinic acid and Baylis-Hillman reaction-derived allylic alcohols. These alkynes and azides were then coupled under click cycloaddition conditions to obtain functionalized betulinic acid-triazole conjugates. Similarly, pyrazinyl- and indolylbetulinic acid-triazoles were also prepared employing cycloaddition chemistry. All the synthetic compounds were tested for their cytotoxicity against murine breast cancer (4T1) and human pancreatic cancer (MIA PaCa-2) cell lines. Based on these in vitro assays, two series of compounds have been identified as lead compounds for further development.
Keywords
- Betulin,
- Betulinic acid,
- Baylis-Hillman reaction,
- Click reaction,
- Triazole,
- Cycloaddition
Disciplines
Publication Date
2016
DOI
10.1016/j.tet.2016.11.056
Citation Information
Pathi Suman, Amardeep Patel, Lucas Solano, Gayathri Jampana, et al.. "Synthesis and cytotoxicity of Baylis-Hillman template derived betulinic acid-triazole conjugates" Tetrahedron (2016) ISSN: 0040-4020 Available at: http://works.bepress.com/subash-jonnalagadda/1/