1448314-11-1Relevant academic research and scientific papers
A novel reactive turn-on probe capable of selective profiling and no-wash imaging of Bruton's tyrosine kinase in live cells
Wang, Xin,Ma, Nan,Wu, Rui,Ding, Ke,Li, Zhengqiu
supporting information, p. 3473 - 3476 (2019/03/26)
Bruton's tyrosine kinase, an essential mediator of B cell receptor (BCR) signalling, has been validated as an effective therapeutic target in oncology. Development of chemical sensors capable of precise detection of its expression and function is of great
Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents
Gurrapu, Shirisha,Jonnalagadda, Sravan K.,Alam, Mohammad A.,Ronayne, Conor T.,Nelson, Grady L.,Solano, Lucas N.,Lueth, Erica A.,Drewes, Lester R.,Mereddy, Venkatram R.
, p. 3282 - 3286 (2016/07/12)
Novel N,N-dialkyl carboxy coumarins have been synthesized as potential anticancer agents via inhibition of monocarboxylate transporter 1 (MCT1). These coumarin carboxylic acids have been evaluated for their in vitro MCT1 inhibition, MTT cancer cell viability, bidirectional Caco-2 cell permeability, and stability in human and liver microsomes. These results indicate that one of the lead candidate compounds 4a has good absorption, metabolic stability, and a low drug efflux ratio. Systemic toxicity studies with lead compound 4a in healthy mice demonstrate that this inhibitor is well tolerated based on zero animal mortality and normal body weight gains compared to the control group. In vivo tumor growth inhibition studies in mice show that the candidate compound 4a exhibits significant single agent activity in MCT1 expressing GL261-luc2 syngraft model but doesn't show significant activity in MCT4 expressing MDA-MB-231 xenograft model, indicating the selectivity of 4a for MCT1 expressing tumors.
