Russian journal of bioorganic chemistry2022,Vol.48Issue(3) :8.DOI:10.1134/S1068162022030062

Design, Synthesis, and Antitumor Activity of New N4-Alkyl-N2-Phenyl-Pyrrolo[3,2-d]Pyrimidine-2,4-Diamine Derivatives as CDK6 Inhibitors

Huang, Chuanhui Wang, Shan Ma, Weifeng
Russian journal of bioorganic chemistry2022,Vol.48Issue(3) :8.DOI:10.1134/S1068162022030062

Design, Synthesis, and Antitumor Activity of New N4-Alkyl-N2-Phenyl-Pyrrolo[3,2-d]Pyrimidine-2,4-Diamine Derivatives as CDK6 Inhibitors

Huang, Chuanhui 1Wang, Shan 1Ma, Weifeng2
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作者信息

  • 1. Xinyang Vocat & Tech Coll
  • 2. Zhengzhou Univ
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Abstract

In this study, a series of new N4-alkyl-N2-phenyl-pyrrolo[3,2-d]pyrimidine-2,4-diamine derivatives has been designed and synthesized. The anti-proliferative activities of these compounds were evaluated against human breast cancer cells and human gastric cancer cells. The CDK6 inhibitory activities of these compounds were tested as well. The most potent compound (IVj) showed super antitumor activities than the positive control palbociclib and good CDK6 inhibitory activity. The probable binding model of (IVj) with CDK6 was simulated by molecular docking.

Key words

CDK inhibitor/synthesis/pyrrolo[3/2-d] pyrimidine/antitumor/molecular docking/KINASE 4/6 INHIBITORS/CYCLIN/PALBOCICLIB/RESISTANCE/RIBOCICLIB

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出版年

2022
Russian journal of bioorganic chemistry

Russian journal of bioorganic chemistry

SCI
ISSN:1068-1620
参考文献量23
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