Li, Deping; Liu, Wenwu; Huang, Yaoguan; Liu, Mingyue; Tian, Caizhi; Lu, Hongyuan; Jia, Hui; Xu, Zihua; Ding, Huaiwei; Zhao, Qingchun published the artcile< Facile synthesis of C1-substituted β-carbolines as CDK4 inhibitors for the treatment of cancer>, Quality Control of 3731-53-1, the main research area is beta carboline preparation SAR antitumor human CDK4 inhibitor; CDK4; HCT116; Harmine; β-carboline.
Cyclin-dependent kinase 4 (CDK4), which is involved in dynamic regulation of cell cycle, has gained particularly attention for its role in controlling tumor growth. Increasing evidence showed that β-carboline derivatives have the potential to inhibit CDK4. Herein, on the basis of previous work, authors designed and synthesized a series of novel β-carbolines and evaluated their antitumor activity. Among them, compounds I and II, with the most potent anti-proliferative activity and CDK4 enzymic inhibition activity, were selected for further pharmacol. research in vitro and in vivo. The results in vitro showed that I and II exhibited potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. In vivo, I showed significant tumor growth inhibition in HCT116 tumor xenograft model without causing significant weight loss and toxicity consistent with the acute toxicity test. In addition, silico study showed I and II not only have good biol. actions, but also acceptable predicted ADME and physicochem. properties. Taken together, compounds I and II could be selected for further modification and preclin. evaluation.
Bioorganic Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Quality Control of 3731-53-1.