Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 5, Pages 1297-1301Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.12.098
Keywords
Curcumin derivatives; Antitumor; Antioxidant activity; Aqueous solubility
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Funding
- National Natural Science Foundation of China [81001361, 20971022]
- Ph.D. Programs Foundation of Ministry of Education of China [20100092120046]
- Open Project Program of State Key Laboratory of Natural Medicines, China Pharmaceutical University
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A series of dimethylaminomethyl-substituted curcumin derivatives/analogues were designed and synthesized. All compounds effectively inhibited HepG2, SGC-7901, A549 and HCT-116 tumor cell lines proliferation in MTT assay. Particularly, compounds 2a and 3d showed much better activity than curcumin against all of the four tumor cell lines. Antioxidant test revealed that these compounds had higher free radical scavenging activity than curcumin towards both DPPH and galvinoxyl radicals. Furthermore, the aqueous solubility and stability of the target compounds were also significantly improved compared with curcumin. (c) 2013 Elsevier Ltd. All rights reserved.
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