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12-Amino-andrographolide analogues: synthesis and cytotoxic activity. 2013
Sakkasem Kasemsuk, and
Uthaiwan Sirion, and
Kanoknetr Suksen, and
Pawinee Piyachaturawat, and
Apichart Suksamrarn, and
Rungnapha Saeeng
Department of Chemistry and Center for Innovation in Chemistry, Faculty of Science, Burapha University, Chonburi, 20131, Thailand.
Andrographolide, a diterpenoid lactone of the plant Andrographis paniculata, has been shown to be cytotoxic against various cancer cells in vitro. In the present study, a series of β-amino-γ-butyrolactone analogues has been synthesized from naturally occurring andrographolide via one pot tandem aza-conjugate addition-elimination reaction. By using economic procedure without any base or catalyst at room temperature, the products obtained were in fair to excellent yields with high stereoselectivity. The cytotoxicity of all new amino analogues were evaluated against six cancer cell lines and revealed their potential for being developed as promising anti-cancer agents.
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