3,6-取代-9-吡啶甲基咔唑類衍生物對於HL-60細胞分化作用之影響; Effect of 3,6-subsituted 9- pyridylmethylcarbazole derivatives on differentiation of HL-60 cells

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题名:	3,6-取代-9-吡啶甲基咔唑類衍生物對於HL-60細胞分化作用之影響;Effect of 3,6-subsituted 9- pyridylmethylcarbazole derivatives on differentiation of HL-60 cells
作者:	馮鈞達;Feng Chun-Ta
贡献者:	中國醫藥大學藥物化學研究所
日期:	1993
上传时间:	2009-12-24 11:01:19 (UTC+8)
摘要:	為了尋找能夠有效誘導白血病細胞分化之化合物，著者篩選了一系列之3,6-取代-9-吡啶甲基咔唑類衍生物以進行誘導細胞分化作用及抑制細胞增殖作用之活性測試。由實驗結果發現化合物HYL-3b單獨使用時之分化效果最為顯著，而併用全反式維甲酸之後的分化效果也有很好的效果。於是進ㄧ步以其對於細胞週期之影響來探討初步機轉。 HYL-3b單獨使用之實驗結果發現細胞週期停留於G0/ G1期-與全反式維甲酸相似。由此可知，HYL-3b可望成為新一類型之急性前骨髓性白血病治療藥物。; In order to develop the novel leukemia cell differentiation agents, a series of 3,6-subsituted 9-pyridylmethylcarbazole derivatives was been screened for their induced differentiation and growth inhibition activities of HL-60 cells. According to the results, when using compound HYL-3b along, it was the most effective to differentiation compared with the other compounds. And it is shown the great coefficient effect to differentiation when combined with all-trans retinoic acid (ATRA). Therefore, the further studies of action mechanism were carried out to evaluate its effects on the cell cycle of HL-60 cells. When treatment of compound HYL-3b alone, it was found to affect the cell cycle as the same way of ATRA, which induced G0/ G1 phase arrest of HL-60 cells. This finding suggests that compound HYL-3b maybe has great potential in the treatment of acute promyelocytic leukemia (APL) either dose alone or together with ATRA.
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