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2015 | 62 | 3 | 547-552
Article title

Synthesis of kaempferide Mannich base derivatives and their antiproliferative activity on three human cancer cell lines

Content
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EN
Abstracts
EN
Kaempferide (3,5,7-trihydroxy-4'-methoxyflavone, 1), a naturally occurring flavonoid with potent anticancer activity in a number of human tumour cell lines, was first semisynthesized from naringin. Based on Mannich reaction of kaempferide with various secondary amines and formaldehyde, nine novel kaempferide Mannich base derivatives 2-10 were synthesized. The aminomethylation occurred preferentially in the position at C-6 and C-8 of the A-ring of kaempferide. All the synthetic compounds were tested for antiproliferative activity against three human cancer cell lines (Hela, HCC1954, SK-OV-3) by the standard MTT method. The results showed that compounds 1, 2 and 5-10 were more potent against Hela cells with IC50 values of 12.47-28.24 μM than the positive control cis-platin (IC50 41.25 μM), compounds 5, 6, 8 and 10 were more potent against HCC1954 cells with IC50 values of 8.82-14.97 μM than the positive control cis-platin (IC50 29.68 μM), and compounds 2, 3, 5, 6 and 10 were more potent against SK-OV-3 cells with IC50 values of 7.67-18.50 μM than the positive control cis-platin (IC50 21.27 μM).
Publisher

Year
Volume
62
Issue
3
Pages
547-552
Physical description
Dates
published
2015
received
2015-02-13
revised
2015-04-18
accepted
2015-08-31
(unknown)
2015-09-08
Contributors
  • College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, P R China
  • Faculty of Chemical Engineering, Industry University of Hochiminh City, Vietnam
author
  • College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, P R China
  • College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, P R China
author
  • College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, P R China
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Document Type
Publication order reference
Identifiers
YADDA identifier
bwmeta1.element.bwnjournal-article-abpv62p547kz
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