Monocarboxylate Transporter 1 Inhibitors as Potential Anticancer Agents
journal contributionposted on 14.05.2015, 00:00 by Shirisha Gurrapu, Sravan K. Jonnalagadda, Mohammad A. Alam, Grady L. Nelson, Mary G. Sneve, Lester R. Drewes, Venkatram R. Mereddy
Potent monocarboxylate transporter 1 inhibitors (MCT1) have been developed based on α-cyano-4-hydroxycinnamic acid template. Structure–activity relationship studies demonstrate that the introduction of p-N, N-dialkyl/diaryl, and o-methoxy groups into cyanocinnamic acid has maximal MCT1 inhibitory activity. Systemic toxicity studies in healthy ICR mice with few potent MCT1 inhibitors indicate normal body weight gains in treated animals. In vivo tumor growth inhibition studies in colorectal adenocarcinoma (WiDr cell line) in nude mice xenograft models establish that compound 27 exhibits single agent activity in inhibiting the tumor growth.
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ICR miceagent activityvivo tumor growth inhibition studiescompound 27 exhibitsmice xenograft modelsMCT 1 inhibitorsMonocarboxylate Transporter 1 InhibitorsSystemic toxicity studiescolorectal adenocarcinomabody weight gainsMCT 1cyanocinnamic acidPotential Anticancer AgentsPotent monocarboxylate transporter 1 inhibitorstumor growthWiDr cell line