Synthesis and evaluation of curcumin-related compounds for anticancer activity

Xingchuan Wei, Zhi Yun Du, Xi Zheng, Xiao Xing Cui, Allan H. Conney, Kun Zhang

Research output: Contribution to journalArticlepeer-review

79 Scopus citations

Abstract

Sixty-one curcumin-related compounds were synthesized and evaluated for their anticancer activity toward cultured prostate cancer PC-3 cells, pancreas cancer Panc-1 cells and colon cancer HT-29 cells. Inhibitory effects of these compounds on the growth of PC-3, Panc-1 and HT-29 cells were determined by the MTT assay. Compounds E10, F10, FN1 and FN2 exhibited exceptionally potent inhibitory effects on the growth of cultured PC-3, Panc-1 and HT-29 cells. The IC50 for these compounds was lower than 1 μM in all three cell lines. E10 was 72-, 46- and 117-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. F10 was 69-, 34- and 72-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. FN1 and FN2 had about the same inhibitory effect as E10 and F10 toward Panc-1 cells but were less active than E10 and F10 toward PC-3 and HT-29 cells. The active compounds were potent stimulators of apoptosis. The present study indicates that E10, F10, FN1 and FN2 may have useful anticancer activity.

Original languageEnglish (US)
Pages (from-to)235-245
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume53
DOIs
StatePublished - Jul 1 2012

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Keywords

  • Anticancer curcumin derivatives
  • Inhibition of colon cancer
  • Inhibition of pancreas cancer
  • Inhibition of prostate cancer

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