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Literature DB >> 20932759

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

Italo Beria¹, Barbara Valsasina, Maria Gabriella Brasca, Walter Ceccarelli, Maristella Colombo, Sabrina Cribioli, Gabriele Fachin, Ronald D Ferguson, Francesco Fiorentini, Laura M Gianellini, Maria L Giorgini, Jurgen K Moll, Helena Posteri, Daniele Pezzetta, Fulvia Roletto, Francesco Sola, Dania Tesei, Michele Caruso.

Abstract

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.

Entities: Chemical Disease Gene

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Year: 2010 PMID： 20932759 DOI： 10.1016/j.bmcl.2010.09.060

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

6 in total

Review 1. In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases.

Authors: C I Wells; N R Kapadia; R M Couñago; D H Drewry
Journal: Medchemcomm Date: 2017-12-08 Impact factor: 3.597

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

Review 1. In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases.

2. Synthesis of Trifluoromethoxylated (Hetero)Arenes via OCF₃ Migration.

Review 3. Applications of Palladium-Catalyzed C-N Cross-Coupling Reactions.

4. Mechanistic studies on intramolecular C-H trifluoromethoxylation of (hetero)arenes via OCF3-migration.

5. Combined pharmacophore modeling, docking, and 3D-QSAR studies of PLK1 inhibitors.

6. Identification and antitumor activity of a novel inhibitor of the NIMA-related kinase NEK6.

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

Review 1. In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases.

2. Synthesis of Trifluoromethoxylated (Hetero)Arenes via OCF3 Migration.

Review 3. Applications of Palladium-Catalyzed C-N Cross-Coupling Reactions.

4. Mechanistic studies on intramolecular C-H trifluoromethoxylation of (hetero)arenes via OCF3-migration.

5. Combined pharmacophore modeling, docking, and 3D-QSAR studies of PLK1 inhibitors.

6. Identification and antitumor activity of a novel inhibitor of the NIMA-related kinase NEK6.

2. Synthesis of Trifluoromethoxylated (Hetero)Arenes via OCF₃ Migration.