Relationship Between the Structure of Methoxylated and Hydroxylated Flavones and Their Antiproliferative Activity in HL60 Cells

Satoru Kawaii; Yuya Ishikawa; Yuko Yoshizawa

doi:10.21873/anticanres.12904

Relationship Between the Structure of Methoxylated and Hydroxylated Flavones and Their Antiproliferative Activity in HL60 Cells

Anticancer Res. 2018 Oct;38(10):5679-5684. doi: 10.21873/anticanres.12904.

Authors

Satoru Kawaii¹, Yuya Ishikawa², Yuko Yoshizawa³

Affiliations

¹ Laboratory of Bio-organic Chemistry, Tokyo Denki University, Saitama, Japan kawaii@mail.dendai.ac.jp.
² Laboratory of Bio-organic Chemistry, Tokyo Denki University, Saitama, Japan.
³ Laboratory of Bio-organic Chemistry, Akita Prefectural University, Akita, Japan.

PMID: 30275187
DOI: 10.21873/anticanres.12904

Abstract

As part of our continuing investigation on flavonoid derivatives as potential anticancer substances, a series of methoxylated and hydroxylated flavones was synthesized, and their cytotoxic and anti-proliferative activity was evaluated in leukemic HL60 cells. Their structure-activity relationship was also investigated. The correlation between the methoxylation/hydroxylation pattern and antiproliferative activity revealed the importance of the 5,4'- and 3',4'-dihydroxyl moieties in flavone nucleus.

Keywords: HL60 cells; Methoxyflavone; antiproliferative activity; hydroxyflavone; structure and activity relationship.

MeSH terms

Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology*
Cell Proliferation / drug effects*
Drug Screening Assays, Antitumor
Flavones / chemistry*
Flavones / pharmacology*
HL-60 Cells
Humans
Structure-Activity Relationship

Substances

Antineoplastic Agents
Flavones