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Research ArticleExperimental Studies

Relationship between Structure and Antiproliferative Activity of Polymethoxyflavones towards HL60 Cells

SATORU KAWAII, TOMOYASU IKUINA, TAKESHI HIKIMA, TETSUO TOKIWANO and YUKO YOSHIZAWA
Anticancer Research December 2012, 32 (12) 5239-5244;
SATORU KAWAII
1Laboratory of Bio-organic Chemistry, Tokyo Denki University, Hatoyama, Saitama, Japan
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  • For correspondence: kawaii@mail.dendai.ac.jp
TOMOYASU IKUINA
1Laboratory of Bio-organic Chemistry, Tokyo Denki University, Hatoyama, Saitama, Japan
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TAKESHI HIKIMA
1Laboratory of Bio-organic Chemistry, Tokyo Denki University, Hatoyama, Saitama, Japan
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TETSUO TOKIWANO
2Laboratory of Bio-organic Chemistry, Akita Prefectural University, Akita, Japan
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YUKO YOSHIZAWA
2Laboratory of Bio-organic Chemistry, Akita Prefectural University, Akita, Japan
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Abstract

As part of our continuing investigation of polymethoxyflavone (PMF) derivatives as potential anticancer substances, a series of PMF derivatives was synthesized. The synthesized compounds were evaluated for cytotoxicity against the promyelocytic leukemic HL60 cell line, and structure–activity relationship correlations were investigated along with previously isolated PMFs from the peel of king orange (Citrus nobilis). 7,3’-Dimethoxyflavone demonstrated the most potent activity among the synthetic PMFs. Consideration of correlation between the methoxylation pattern and antiproliferative activity revealed the importance of the 3’-methoxyl group and the higher degree of methoxylation on the A-ring moiety of PMFs.

  • Polymethoxylated flavone
  • antiproliferative activity
  • HL60 cells
  • structure and activity relationship
  • Received September 25, 2012.
  • Revision received October 26, 2012.
  • Accepted October 29, 2012.
  • Copyright© 2012 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved
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Anticancer Research: 32 (12)
Anticancer Research
Vol. 32, Issue 12
December 2012
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Relationship between Structure and Antiproliferative Activity of Polymethoxyflavones towards HL60 Cells
SATORU KAWAII, TOMOYASU IKUINA, TAKESHI HIKIMA, TETSUO TOKIWANO, YUKO YOSHIZAWA
Anticancer Research Dec 2012, 32 (12) 5239-5244;

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Relationship between Structure and Antiproliferative Activity of Polymethoxyflavones towards HL60 Cells
SATORU KAWAII, TOMOYASU IKUINA, TAKESHI HIKIMA, TETSUO TOKIWANO, YUKO YOSHIZAWA
Anticancer Research Dec 2012, 32 (12) 5239-5244;
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Keywords

  • Polymethoxylated flavone
  • antiproliferative activity
  • HL60 cells
  • structure and activity relationship
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