Abstract：
:Based on the fact that timosaponin A-III (TA-III) exhibits potent cytotoxic effects and has been considered as a potential anti-tumor agent, a range of novel sarsasapogenin derivatives 1, 2a-2g, 3, 4, 5, 6a-6g have been synthesized by a simple and facile synthetic route. The in vitro cytotoxic activity of these synthetic compounds has been evaluated against ten human cancer cell lines. The pharmacological results showed that most of the sarsasapogenin derivatives displayed excellent selective cytotoxicity toward the cancer cell lines. An amino group at C-3 or C-26 position of the sapogenin had a profound influence on the cytotoxic activity. In particular, compound 6c exhibited significantly inhibitory activity against A375-S2 (IC50=0.56μM) and HT1080 (IC50=0.72μM) cells. However, introducing a bromo or morpholinyl substituent at the C-3 and C-26 position of the sapogenin generally rendered it inactive against the human cancer cell lines. This research provides a theoretical reference for the exploration of new anti-tumor drugs.
journal_name
Steroidsjournal_title
Steroidsauthors
Yin Y,Zhao XC,Wang SJ,Gao PY,Li LZ,Ikejima T,Song SJdoi
10.1016/j.steroids.2014.09.007subject
Has Abstractpub_date
2015-01-01 00:00:00pages
25-31eissn
0039-128Xissn
1878-5867pii
S0039-128X(14)00253-0journal_volume
93pub_type
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