Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592950 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
Forty four di- or trisubstituted novel isatin derivatives were designed and synthesized in 5-6 steps in 25-45% overall yields. Their structures were confirmed by 1H NMR and 13C NMR as well as LC-MS. The anticancer activity of these new isatin derivatives against three human tumor cell lines, K562, HepG2 and HT-29, were evaluated by MTT assay in vitro. SAR studies suggested that the combination of 1-benzyl and 5-[trans-2-(methoxycarbonyl)ethen-1-yl] substitution greatly enhance their cytotoxic activity, whereas an intact carbonyl functionality on C-3 as present in the parent ring is required to such a potency. This study leads to the identification of two highly active molecules, compounds 2h (IC50Â =Â 3Â nM) and 2k (IC50Â =Â 6Â nM), against human leukemia K562 cells.
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Authors
Kailin Han, Yao Zhou, Fengxi Liu, Qiannan Guo, Pengfei Wang, Yao Yang, Binbin Song, Wei Liu, Qingwei Yao, Yuou Teng, Peng Yu,