Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant--taxoid conjugates as novel cytotoxic agents.

Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant--taxoid conjugates as novel cytotoxic agents. Research Abstract Details 

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Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant--taxoid conjugates as novel cytotoxic agents. Abstract Text:

Kyoko Nakagawa-Goto,Koji Yamada,Seikou Nakamura,Tzu-Hsuan Chen,Po-Cheng Chiang,Kenneth F Bastow,Shao-Chun Wang,Bill Spohn,Mien-Chie Hung,Fang-Yu Lee,Fang-Chen Lee,Kuo-Hsiung Lee,Kyoko Nakagawa-Goto,Koji Yamada,Seikou Nakamura,Tzu-Hsuan Chen,Po-Cheng Chiang,Kenneth F Bastow,Shao-Chun Wang,Bill Spohn,Mien-Chie Hung,Fang-Yu Lee,Fang-Chen Lee,Kuo-Hsiung Lee,

Various dietary antioxidants, including vitamins, flavonoids, curcumin, and a coumarin, were conjugated with paclitaxel (1) through an ester linkage. The newly synthesized compounds were evaluated for cytotoxic activity against several human tumor cell lines as well as the corresponding normal cell lines. Interestingly, most tested conjugates selectively inhibited the growth of 1A9 (ovarian) and KB (nasopharyngeal) tumor cells without activity against other cell lines. Particularly, conjugates 16 and 20 were highly active against 1A9 (ED(50) value of 0.005 microg/mL) as well as KB (ED(50) values of 0.005 and 0.14 microg/mL, respectively) cells. Compound 22b, the glycinate ester salt of vitamin E conjugated with 1, appears to be a promising lead for further development as a clinical trial candidate as it exhibited strong inhibitory activity against Panc-1 (pancreatic cancer) with less effect on the related E6E7 (normal) cell line.

Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant--taxoid conjugates as novel cytotoxic agents. Publishing Authors By Initials

K Nakagawa-Goto,K Yamada,S Nakamura,TH Chen,PC Chiang,KF Bastow,SC Wang,B Spohn,MC Hung,FY Lee,FC Lee,KH Lee,K Nakagawa-Goto,K Yamada,S Nakamura,TH Chen,PC Chiang,KF Bastow,SC Wang,B Spohn,MC Hung,FY Lee,FC Lee,KH Lee,

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Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant--taxoid conjugates as novel cytotoxic agents. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 5204-9

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 4

MONTH: 07

YEAR: 2007

Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant--taxoid conjugates as novel cytotoxic agents. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant--taxoid conjugates as novel cytotoxic agents.

AFFILIATION: Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.

Country: England

AGENCY: United States NCI

GRANT: CA17525

ACRONYM: CA

MEDLINETA: Bioorg Med Chem Lett

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