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.
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Natl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Safety Evaluat, Shanghai 200031, Peoples R ChinaNatl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
Luan, Yang
Kogi, Mieko
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Natl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
Kanazawa Inst Technol, Dept Appl Biosci, Coll Biosci & Chem, Kanazawa, Ishikawa 9240838, JapanNatl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
Kogi, Mieko
Rajaguru, Palanisamy
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Natl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
Anna Univ Technol, Dept Biotechnol, Tiruchirappalli 620024, IndiaNatl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
Rajaguru, Palanisamy
Ren, Jin
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Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Safety Evaluat, Shanghai 200031, Peoples R ChinaNatl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
Ren, Jin
Yamaguchi, Teruhide
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Natl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, JapanNatl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
Yamaguchi, Teruhide
Suzuki, Kazuhiro
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Natl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, JapanNatl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
Suzuki, Kazuhiro
Suzuki, Takayoshi
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Natl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, JapanNatl Inst Hlth Sci, Div Cellular & Gene Therapy Prod, Setagaya Ku, Tokyo 1588501, Japan
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Tokyo Denki Univ, Sch Sci & Engn, Div Life Sci & Engn, Hatoyama, Saitama 3500394, JapanTokyo Denki Univ, Sch Sci & Engn, Div Life Sci & Engn, Hatoyama, Saitama 3500394, Japan
Nagahara, Yukitoshi
Nagahara, Katsuhiko
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Kitasato Univ, Dept Pharmaceut Life Sci, Fac Pharm, Tokyo, JapanTokyo Denki Univ, Sch Sci & Engn, Div Life Sci & Engn, Hatoyama, Saitama 3500394, Japan