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Open AccessArticle

Synthesis and Biological Evaluation of Novel Curcuminoid Derivatives

by Ya-Kun Cao 1,†, Hui-Jing Li 2,†, Zhi-Fang Song 1, Yang Li 1 and Qi-Yong Huai 1,*
1
Department of Applied Chemistry, Marine College, Shandong University, Weihai 264209, China
2
Department of Environmental Engineering, School of Marine Science and Technology, Harbin Institute of Technology, Weihai 264209, China
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2014, 19(10), 16349-16372; https://doi.org/10.3390/molecules191016349
Received: 15 September 2014 / Revised: 26 September 2014 / Accepted: 29 September 2014 / Published: 13 October 2014
(This article belongs to the Section Medicinal Chemistry)
Curcuminoids have been reported to possess multiple bioactivities, such as antioxidant, anticancer and anti-inflammatory properties. Three novel series of curcuminoid derivatives (11ah, 15ah and 19ad) with enhanced bioactivity have been synthesized. Among the synthesized compounds, 11b exhibited the most significant activity with an MIC of 0.5 µM /mL against selected medically important Gram-positive cocci (S. aureus and S. viridans) and Gram-negative bacilli (E. coli and E. cloacae). The derivatives exhibited remarkable results in an antioxidant test with an IC50 2.4- to 9.3-folder smaller than curcuminoids. With respect to antiproliferative activity against Hep-G2, LX-2, SMMC7221 and MDA-MB-231, the derivatives exhibited an effect stronger than curcuminoids with an IC50 ranging from 0.18 to 4.25 µM. View Full-Text
Keywords: curcuminoids; antibacterial; antioxidant; antiproliferative curcuminoids; antibacterial; antioxidant; antiproliferative
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MDPI and ACS Style

Cao, Y.-K.; Li, H.-J.; Song, Z.-F.; Li, Y.; Huai, Q.-Y. Synthesis and Biological Evaluation of Novel Curcuminoid Derivatives. Molecules 2014, 19, 16349-16372.

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