杂环双芳基嘌呤衍生物作为有效的抗增殖剂：细胞周期蛋白依赖性激酶抑制剂。第二部分。
Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II.
机构信息
AMRI, Medicinal Chemistry Department, 26 Corporate Circle, Albany, NY 12212-5098, USA.
出版信息
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6613-7. doi: 10.1016/j.bmcl.2009.10.011. Epub 2009 Oct 12.
C-6 Biarylmethylamino purine derivatives of roscovitine (1) inhibit cyclin dependent kinases and demonstrate potent antiproliferative activity. Replacement of the aryl rings of the C-6 biarylmethylamino group with heterobiaryl rings has provided compounds with significantly improved activity. In particular, derivatives 18 g and 9 c demonstrated 1000-fold and 1250-fold improvements, respectively, in the growth inhibition of HeLa cells compared to roscovitine (1).
C-6 双芳基甲氨基嘌呤衍生物的罗斯考维汀（1）抑制细胞周期依赖性激酶，并表现出很强的抗增殖活性。用杂芳基环取代 C-6 双芳基甲氨基的芳基环，提供了活性显著提高的化合物。特别是，衍生物 18 g 和 9 c 与罗斯考维汀（1）相比，对 HeLa 细胞生长的抑制作用分别提高了 1000 倍和 1250 倍。
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