Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity was written by Liu, Yinyin;Xia, Qinhua;Fang, Lei. And the article was included in Bioorganic & Medicinal Chemistry in 2018.Application of 1009303-77-8 This article mentions the following:
Using pyridino[2,3-D]pyrimidine as the core, total 13 pyridino[2,3-D]pyrimidine derivatives with different alkyl substituents at C2 site have been designed and synthesized to search for novel PI3Kα/mTOR dual inhibitors. Most of the target compounds showed potent mTOR inhibition activity with IC50 values ranging from single to double digit nanomole. Five target compounds exhibited pronounced PI3Kα inhibition activity. In vitro cellular assay indicated that most of the target compounds showed excellent antiproliferative activity, especially I whose potency against SKOV3 was 8-fold higher than the pos. control AZD8055. In vitro metabolic stability study found that I had a comparable stability to that of AZD8055. More importantly, I showed better antitumor activity and pharmacokinetic properties in vivo as compared with AZD8055. In the experiment, the researchers used many compounds, for example, 2-Methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzenemethanol (cas: 1009303-77-8Application of 1009303-77-8).
2-Methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzenemethanol (cas: 1009303-77-8) belongs to ethers. Ether is less polar than esters, alcohols or amines because of the oxygen atom that is unable to participate in hydrogen bonding due to the presence of bulky alkyl groups on both sides of the oxygen atom. But ether is more polar than alkenes. Autoxidation is the spontaneous oxidation of a compound in air. In the presence of oxygen, ethers slowly autoxidize to form hydroperoxides and dialkyl peroxides. If concentrated or heated, these peroxides may explode. To prevent such explosions, ethers should be obtained in small quantities, kept in tightly sealed containers, and used promptly.Application of 1009303-77-8
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem