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Recent Advances in the Discovery and Development of Flavonoids and their Analogues as Antitumor and Anti-HIV Agents

  • Chapter
Flavonoids in the Living System

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 439))

Abstract

Antitumor and anti-HIV flavonoids and their analogues will be reviewed with emphasis on those discovered in our laboratory. The active antitumor compounds include the antileukemic tricin (1) and kaempferol-3-O-β-D-glucopyranoside (2) from Wikstroemia indica, the cytotoxic hinokiflavone (3) from Rhus succedanea, the cytotoxic isoflavone (8) from Amorpha fruticosa, two dihydroxypentamethoxyflavones (9, 10) from Polanisia dodencandra. The development of synthetic 2-phenyI-4-quinolones as potent cytotoxic antimitotic flavonoid analogues and 2-phenylthiochromen-4-ones as potent antitumor flavonoid analogues will be presented. Selected results from other laboratories and antitumor-related biological studies also will be discussed. Flavonoids have also been investigated as potential anti-HIV agents. In our laboratory, acacetin-7-O-β-D-galactopyranoside (131) from Chrysanthemum morifolium and chrysin (102), as well as apigenin-7-O-β-D-glucopyranoside (130), from Kummerowia striata, have been found to exhibit anti-HIV activity. In other studies, some flavonoids and related compounds have been investigated as inhibitors of HIV-1 reverse transcriptase, protease, and integrase. The isolation and structural modification of such plant-derived active principles provide a continuing source of potential antitumor and anti-HIV agents.

Antitumor agents 179. For 178, see Chen, K.; Kuo, S. C; Mauger, A.; Lin, C. M.; Hamel, E.; and Lee, K. H. Synthesis and biological evaluation of substituted 2-aryl-l,8-naphthyridin-4-ones as antitumor agents that inhibit tubulin polymerization. J. Med. Chem. 1997, 40, 3049-3056.

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Authors and Affiliations

  1. Natural Products Laboratory Division of Medicinal Chemistry and Natural Products, School of Pharmacy University of North Carolina, Chapel Hill, North Carolina, 27599, USA

    Hui-Kang Wang, Yi Xia, Zheng-Yu Yang, Susan L. Morris Natschke & Kuo-Hsiung Lee

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  1. Hui-Kang Wang
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  2. Yi Xia
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  3. Zheng-Yu Yang
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  4. Susan L. Morris Natschke
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  5. Kuo-Hsiung Lee
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Editors and Affiliations

  1. United States Department of Agriculture, Citrus and Subtropical Products Laboratory, P.O. Box 1909, 33883, Winter Haven, Florida, USA

    John A. Manthey

  2. State of Florida Department of Citrus, 700 Experiment Station Road, Lake Alfred, Florida, 33850, USA

    Béla S. Buslig

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Wang, HK., Xia, Y., Yang, ZY., Morris Natschke, S.L., Lee, KH. (1998). Recent Advances in the Discovery and Development of Flavonoids and their Analogues as Antitumor and Anti-HIV Agents. In: Manthey, J.A., Buslig, B.S. (eds) Flavonoids in the Living System. Advances in Experimental Medicine and Biology, vol 439. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-5335-9_15

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