1069113-47-8Relevant academic research and scientific papers
Polycyclic amide derivative as CDK9 inhibitor, and preparation method and application thereof
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Paragraph 0353-0356; 0360-0362, (2021/07/24)
The invention belongs to the technical field of polycyclic amide derivatives, and particularly relates to a polycyclic amide derivative as a CDK9 inhibitor, and a preparation method and application thereof. The polycyclic amide derivative shows excellent CDK9 enzyme inhibitory activity, and can be used for preparing drugs for treating cancers, especially hematologic cancers including acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, follicular lymphoma and the like and solid tumors, such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia and follicular lymphoma, including breast cancer, prostate cancer, ovarian cancer, hepatocellular carcinoma, pancreatic cancer, kidney cancer, stomach cancer, colorectal cancer, lung cancer and the like.
Novel nicotinic acetylcholine receptor agonists containing carbonyl moiety as a hydrogen bond acceptor
Mazurov, Anatoly A.,Kombo, David C.,Akireddy, Srinivasa,Murthy, Srinivasa,Hauser, Terry A.,Jordan, Kristen G.,Gatto, Gregory J.,Yohannes, Daniel
, p. 3927 - 3934 (2013/07/27)
A novel series of α4β2 nAChR agonists lacking common pyridine or its bioisosteric heterocycle have been disclosed. Essential pharmacophoric elements of the series are exocyclic carbonyl moiety as a hydrogen bond acceptor and secondary amino group within diaza- or azabicyclic scaffold. Computer modeling studies suggested that molecular shape of the ligand also contributes to promotion of agonism. Proof of concept for improving working memory performance in a novel object recognition task has been demonstrated on a representative of the series, 3-propionyl-3,7-diazabicyclo[3.3.0]octane (34).
