4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors

Autor:	Michele Caruso, Francesco Fiorentini, Francesco Sola, Maria Laura Giorgini, Laura Gianellini, Italo Beria, Fulvia Roletto, Maria Gabriella Brasca, Maristella Colombo, Barbara Valsasina, Ron Ferguson, Gabriele Fachin, Dania Tesei, Helena Posteri, Jurgen Moll, Walter Ceccarelli, Daniele Pezzetta, Sabrina Cribioli
Rok vydání:	2010
Předmět:	Stereochemistry Clinical Biochemistry Transplantation Heterologous Pharmaceutical Science Cell Cycle Proteins Polo-like kinase Pharmacology Protein Serine-Threonine Kinases Biochemistry PLK1 Structure-Activity Relationship In vivo Cell Line Tumor Proto-Oncogene Proteins Drug Discovery medicine Structure–activity relationship Animals Humans Molecular Biology Protein Kinase Inhibitors Chemistry Kinase Organic Chemistry Transplantation Mechanism of action Cell culture Quinazolines Molecular Medicine medicine.symptom
Zdroj:	Bioorganicmedicinal chemistry letters. 20(22)
ISSN:	1464-3405
Popis:	A series of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives was optimized as Polo-like kinase 1 inhibitors. Extensive SAR afforded a highly potent and selective PLK1 compound. The compound showed good antiproliferative activity when tested in a panel of tumor cell lines with PLK1 related mechanism of action and with good in vivo antitumor efficacy in two xenograft models after i.v. administration.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93859b798e1a9fac70cabff937780dcf https://pubmed.ncbi.nlm.nih.gov/20932759 Zobrazit plný text záznamu Full Text from ScienceDirect