Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents.

Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents. Research Abstract Details 

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Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents. Abstract Text:

Isamu Shiina,Yoshiyuki Sano,Kenya Nakata,Takaaki Kikuchi,Akane Sasaki,Masahiko Ikekita,Yukitoshi Nagahara,Yoshimune Hasome,Takao Yamori,Kanami Yamazaki,Isamu Shiina,Yoshiyuki Sano,Kenya Nakata,Takaaki Kikuchi,Akane Sasaki,Masahiko Ikekita,Yukitoshi Nagahara,Yoshimune Hasome,Takao Yamori,Kanami Yamazaki,

Four pseudo-symmetrical tamoxifen derivatives, RID-B (13), RID-C (14), RID-D (15), and bis(dimethylaminophenetole) (16), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of these pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 13 and 16 strongly inhibit the viability of the HL-60 human acute promyelocytic leukemia cell line, whereas 14 possesses a medium activity against the same cell line and 15 has no effect on the cell viability. The global anti-tumor activity of 13-16 against a variety of human cancer cells was assessed using a panel of 39 human cancer cell lines (JFCR 39), and it was shown that RID-B (13) strongly inhibited the growth of several cancer cell lines at concentrations of less than 1muM (at 0.38muM for SF-539 [central nervous system], at 0.58muM for HT-29 [colon], at 0.20muM for DMS114 [lung], at 0.21muM for LOX-IMVI [melanoma], and at 0.23muM for MKN74 [stomach]).

Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents. Publishing Authors By Initials

I Shiina,Y Sano,K Nakata,T Kikuchi,A Sasaki,M Ikekita,Y Nagahara,Y Hasome,T Yamori,K Yamazaki,I Shiina,Y Sano,K Nakata,T Kikuchi,A Sasaki,M Ikekita,Y Nagahara,Y Hasome,T Yamori,K Yamazaki,

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Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Biochemical pharmacology

VOLUME: 75

Page Numbers: 1014-26

Journal Abbreviation: Biochem. Pharmacol.

ISSN: 0006-2952

DAY: 22

MONTH: 11

YEAR: 2007

Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents. Information

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LANGUAGE: eng

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Grant and Affiliation Information for Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents.

AFFILIATION: Department of Applied Chemistry, Faculty of Science, Tokyo University of Science, Kagurazaka, Shinjuku-ku, Tokyo 162-8601, Japan.

Country: England

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MEDLINETA: Biochem Pharmacol

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