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A novel synthetic analog of 5, 8-disubstituted quinazolines blocks mitosis and induces apoptosis of tumor cells by inhibiting microtubule polymerization.

Tian W, Qin L, Song Q, He L, Ai M, Jin Y, Zhou Z, You S, Long Y, Yu Q - PLoS ONE (2010)

Bottom Line: Tremendous efforts have been made to identify new anti-mitosis compounds for developing more effective and less toxic anti-cancer drugs.In addition, LJK-11 had synergistic effect with another microtubule inhibitor colchicine on blocking mitosis, but not with vinblastine or nocodazole.Understanding the function and mechanism of LJK-11 will help us to better understand the action of anti-microtubule agents and to design better anti-cancer drugs.

View Article: PubMed Central - PubMed

Affiliation: The School of Life Science and Biopharmaceutics of Shenyang Pharmaceutical University, Liaoning, China.

ABSTRACT
Many mitosis inhibitors are powerful anticancer drugs. Tremendous efforts have been made to identify new anti-mitosis compounds for developing more effective and less toxic anti-cancer drugs. We have identified LJK-11, a synthetic analog of 5, 8-disubstituted quinazolines, as a novel mitotic blocker. LJK-11 inhibited growth and induced apoptosis of many different types of tumor cells. It prevented mitotic spindle formation and arrested cells at early phase of mitosis. Detailed in vitro analysis demonstrated that LJK-11 inhibited microtubule polymerization. In addition, LJK-11 had synergistic effect with another microtubule inhibitor colchicine on blocking mitosis, but not with vinblastine or nocodazole. Therefore, LJK-11 represents a novel anti-microtubule structure. Understanding the function and mechanism of LJK-11 will help us to better understand the action of anti-microtubule agents and to design better anti-cancer drugs.

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Effect of LJK-11 on the growth and death of different tumor cells.A549, Hela, HGC-27, or MDA-MB-453 cells were incubated with the indicated concentrations of LJK-11 for 48 hours. The effect of LJK-11 on cell growth and death was evaluated by MTT assay. The cell viability is expressed as a percentage of the compound-treated viable cells divided by the viable cells of the untreated control. The data are the means of triplicates ±SD.
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pone-0010499-g003: Effect of LJK-11 on the growth and death of different tumor cells.A549, Hela, HGC-27, or MDA-MB-453 cells were incubated with the indicated concentrations of LJK-11 for 48 hours. The effect of LJK-11 on cell growth and death was evaluated by MTT assay. The cell viability is expressed as a percentage of the compound-treated viable cells divided by the viable cells of the untreated control. The data are the means of triplicates ±SD.

Mentions: We then analyzed the cell specificity of LJK-11 using human tumor cell lines of different tissue origins, including the lung adenocarcinoma cell line A549, cervical cancer cell line Hela, gastrointestinal cancer cell line HGC-27, and breast cancer cell line MDA-MB-453. Our data indicated that LJK-11 inhibited the growth of A549, Hela, and HGC-27 equally, while had less effect on MDA-MB-453 cells (Fig. 3). These results demonstrated that LJK-11 inhibits growth of most of the tumor cells.


A novel synthetic analog of 5, 8-disubstituted quinazolines blocks mitosis and induces apoptosis of tumor cells by inhibiting microtubule polymerization.

Tian W, Qin L, Song Q, He L, Ai M, Jin Y, Zhou Z, You S, Long Y, Yu Q - PLoS ONE (2010)

Effect of LJK-11 on the growth and death of different tumor cells.A549, Hela, HGC-27, or MDA-MB-453 cells were incubated with the indicated concentrations of LJK-11 for 48 hours. The effect of LJK-11 on cell growth and death was evaluated by MTT assay. The cell viability is expressed as a percentage of the compound-treated viable cells divided by the viable cells of the untreated control. The data are the means of triplicates ±SD.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2864768&req=5

pone-0010499-g003: Effect of LJK-11 on the growth and death of different tumor cells.A549, Hela, HGC-27, or MDA-MB-453 cells were incubated with the indicated concentrations of LJK-11 for 48 hours. The effect of LJK-11 on cell growth and death was evaluated by MTT assay. The cell viability is expressed as a percentage of the compound-treated viable cells divided by the viable cells of the untreated control. The data are the means of triplicates ±SD.
Mentions: We then analyzed the cell specificity of LJK-11 using human tumor cell lines of different tissue origins, including the lung adenocarcinoma cell line A549, cervical cancer cell line Hela, gastrointestinal cancer cell line HGC-27, and breast cancer cell line MDA-MB-453. Our data indicated that LJK-11 inhibited the growth of A549, Hela, and HGC-27 equally, while had less effect on MDA-MB-453 cells (Fig. 3). These results demonstrated that LJK-11 inhibits growth of most of the tumor cells.

Bottom Line: Tremendous efforts have been made to identify new anti-mitosis compounds for developing more effective and less toxic anti-cancer drugs.In addition, LJK-11 had synergistic effect with another microtubule inhibitor colchicine on blocking mitosis, but not with vinblastine or nocodazole.Understanding the function and mechanism of LJK-11 will help us to better understand the action of anti-microtubule agents and to design better anti-cancer drugs.

View Article: PubMed Central - PubMed

Affiliation: The School of Life Science and Biopharmaceutics of Shenyang Pharmaceutical University, Liaoning, China.

ABSTRACT
Many mitosis inhibitors are powerful anticancer drugs. Tremendous efforts have been made to identify new anti-mitosis compounds for developing more effective and less toxic anti-cancer drugs. We have identified LJK-11, a synthetic analog of 5, 8-disubstituted quinazolines, as a novel mitotic blocker. LJK-11 inhibited growth and induced apoptosis of many different types of tumor cells. It prevented mitotic spindle formation and arrested cells at early phase of mitosis. Detailed in vitro analysis demonstrated that LJK-11 inhibited microtubule polymerization. In addition, LJK-11 had synergistic effect with another microtubule inhibitor colchicine on blocking mitosis, but not with vinblastine or nocodazole. Therefore, LJK-11 represents a novel anti-microtubule structure. Understanding the function and mechanism of LJK-11 will help us to better understand the action of anti-microtubule agents and to design better anti-cancer drugs.

Show MeSH
Related in: MedlinePlus