1041015-55-7Relevant academic research and scientific papers
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing
Brasca, Maria Gabriella,Albanese, Clara,Alzani, Rachele,Amici, Raffaella,Avanzi, Nilla,Ballinari, Dario,Bischoff, James,Borghi, Daniela,Casale, Elena,Croci, Valter,Fiorentini, Francesco,Isacchi, Antonella,Mercurio, Ciro,Nesi, Marcella,Orsini, Paolo,Pastori, Wilma,Pesenti, Enrico,Pevarello, Paolo,Roussel, Patrick,Varasi, Mario,Volpi, Daniele,Vulpetti, Anna,Ciomei, Marina
experimental part, p. 1844 - 1853 (2010/05/02)
We have recently reported CDK inhibitors based on the 6-substituted pyrrolo[3,4-c]pyrazole core structure. Improvement of inhibitory potency against multiple CDKs, antiproliferative activity against cancer cell lines and optimization of the physico-chemical properties led to the identification of highly potent compounds. Compound 31 (PHA-793887) showed good efficacy in the human ovarian A2780, colon HCT-116 and pancreatic BX-PC3 carcinoma xenograft models and was well tolerated upon daily treatments by iv administration. It was identified as a drug candidate for clinical evaluation in patients with solid tumors.
CARBONYLAMINO PYRROLOPYRAZOLES, POTENT KINASE INHIBITORS
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Page/Page column 30, (2009/12/28)
Carbonylamino Pyrrolopyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.
