Synthesis of quinolinylaminopyrimidines and quinazolinylmethylaminopyrimidines with antiproliferative activity against melanoma cell line

Jun A Lee; Eun Joo Roh; Chang-Hyun Oh; So Ha Lee; Taebo Sim; Jong Seung Kim; Kyung Ho Yoo

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Synthesis of quinolinylaminopyrimidines and quinazolinylmethylaminopyrimidines with antiproliferative activity against melanoma cell line

机译：对黑色素瘤细胞系具有抗增殖活性的喹啉基氨基嘧啶和喹唑啉基甲基氨基嘧啶的合成

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Synthesis of a new series of quinolinylaminopyrimidines 1a–k and quinazolinylmethylaminopyrimidines 2a–i containing aminoquinoline and aminoquinazoline as hinge regions is described. Their in vitro antiproliferative activities against A375P human melanoma cell line were tested. Among them, compounds 1h and 1k exhibited the highest antiproliferative activities against A375P cell line with IC₅₀ values in sub-micromolar scale. Compounds 1i, 2b and 2g showed similar potency against A375P to Sorafenib as a reference compound. The representative compound 1h showed high, dose-dependent inhibition of MEK and ERK kinases.

机译：合成了一系列新的喹啉基氨基嘧啶1a-k和喹唑啉基甲基氨基嘧啶2a-i，其中含有氨基喹啉和氨基喹唑啉作为铰链区。测试了它们对A375P人黑素瘤细胞系的体外抗增殖活性。其中，化合物1h和1k对A375P细胞株具有最高的抗增殖活性，亚微摩尔级的IC _{50 值。化合物1i，2b和2g对A375P的功效与作为参考化合物的索拉非尼相似。代表性化合物1h对MEK和ERK激酶表现出高度的剂量依赖性抑制作用。}

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《Journal of enzyme inhibition and medicinal chemistry.》 |2015年第4期|共8页
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Jun A Lee; Eun Joo Roh; Chang-Hyun Oh; So Ha Lee; Taebo Sim; Jong Seung Kim; Kyung Ho Yoo;
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1. Synthesis of quinolinylaminopyrimidines and quinazolinylmethylaminopyrimidines with antiproliferative activity against melanoma cell line [J] . Lee Jun A., Roh Eun Joo, Oh Chang-Hyun, Journal of enzyme inhibition and medicinal chemistry. . 2015,第1a6期

机译：对黑色素瘤细胞系具有抗增殖活性的喹啉基氨基嘧啶和喹唑啉基甲基氨基嘧啶的合成
2. Synthesis of 1,2,3-Triazole Benzophenone Derivatives and Evaluation of in vitro Sun Protection, Antioxidant Properties, and Antiproliferative Activity on HT-144 Melanoma Cells [J] . Dias Maria C. F., Sousa Bianca L. de, Ionta Marisa, Journal of the Brazilian Chemical Society . 2021,第3期

机译：1,2,3-三唑二苯甲酮衍生物的合成及其在HT-144黑素瘤细胞上进行体外防晒，抗氧化性能和抗增殖活性的评价
3. Design and synthesis of new imidazo[1,2-a]pyridine and imidazo [1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells [J] . Garamvoelgyi Rita, Dobos Judit, Sipos Anna, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2016,第Null期

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5. Attachment ability and melanoma inhibitory activity mRNA expression level changes in murine B16-F10 melanoma cells post nanosecond electric pulses. [D] . Jia, Hongxia. 2013

机译：纳秒电脉冲后，鼠B16-F10黑色素瘤细胞的附着能力和黑色素瘤抑制活性mRNA表达水平变化。
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7. Synthesis of N-pyridyl azoles using a deprotometalation-iodolysis-N-arylation sequence and evaluation of their antiproliferative activity in melanoma cells [O] . Hedidi, M., Erb, W., Bentabed-Ababsa, G., 2016

机译：利用去金属化-碘解-N-芳基化序列合成N-吡啶基吡咯并评估其在黑素瘤细胞中的抗增殖活性

Synthesis of quinolinylaminopyrimidines and quinazolinylmethylaminopyrimidines with antiproliferative activity against melanoma cell line

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