In 2010,Liu, Kevin K.-C.; Bagrodia, Shubha; Bailey, Simon; Cheng, Hengmiao; Chen, Hui; Gao, Lisa; Greasley, Samantha; Hoffman, Jacqui E.; Hu, Qiyue; Johnson, Ted O.; Knighton, Dan; Liu, Zhengyu; Marx, Matthew A.; Nambu, Mitchell D.; Ninkovic, Sacha; Pascual, Bernadette; Rafidi, Kristina; Rodgers, Caroline M.-L.; Smith, Graham L.; Sun, Shaoxian; Wang, Haitao; Yang, Anle; Yuan, Jing; Zou, Aihua published 《4-Methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Formula: C9H15BN2O2 The information in the text is summarized as follows:
Pteridinones were designed based on a non-selective kinase template. Because of the uniqueness of the PI3K and mTOR binding pockets, a Me group was introduced to C-4 position of the peteridinone core to give compounds with excellent selectivity for PI3K and mTOR. This series of compounds were further optimized to improve their potency against PI3Kα and mTOR. Finally, orally active compounds with improved solubility and robust in vivo efficacy in tumor growth inhibition were identified as well. In the part of experimental materials, we found many familiar compounds, such as 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Formula: C9H15BN2O2)
3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Formula: C9H15BN2O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics