title: Monocarboxylate transporter 1 inhibitors as potential anticancer agents.
abstract: 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.
authors.affiliation: Integrated Biosciences Graduate Program, Department of Chemistry and Biochemistry, Department of Biomedical Sciences, Medical School Duluth, and Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota Duluth , Duluth, Minnesota 55812, United States.
authors.forename: Shirisha
authors.initials: S
authors.lastname: Gurrapu
authors.affiliation: Integrated Biosciences Graduate Program, Department of Chemistry and Biochemistry, Department of Biomedical Sciences, Medical School Duluth, and Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota Duluth , Duluth, Minnesota 55812, United States.
authors.forename: Sravan K
authors.initials: SK
authors.lastname: Jonnalagadda
authors.affiliation: Integrated Biosciences Graduate Program, Department of Chemistry and Biochemistry, Department of Biomedical Sciences, Medical School Duluth, and Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota Duluth , Duluth, Minnesota 55812, United States.
authors.forename: Mohammad A
authors.initials: MA
authors.lastname: Alam
authors.affiliation: Integrated Biosciences Graduate Program, Department of Chemistry and Biochemistry, Department of Biomedical Sciences, Medical School Duluth, and Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota Duluth , Duluth, Minnesota 55812, United States.
authors.forename: Grady L
authors.initials: GL
authors.lastname: Nelson
authors.affiliation: Integrated Biosciences Graduate Program, Department of Chemistry and Biochemistry, Department of Biomedical Sciences, Medical School Duluth, and Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota Duluth , Duluth, Minnesota 55812, United States.
authors.forename: Mary G
authors.initials: MG
authors.lastname: Sneve
authors.affiliation: Integrated Biosciences Graduate Program, Department of Chemistry and Biochemistry, Department of Biomedical Sciences, Medical School Duluth, and Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota Duluth , Duluth, Minnesota 55812, United States.
authors.forename: Lester R
authors.initials: LR
authors.lastname: Drewes
authors.affiliation: Integrated Biosciences Graduate Program, Department of Chemistry and Biochemistry, Department of Biomedical Sciences, Medical School Duluth, and Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota Duluth , Duluth, Minnesota 55812, United States.
authors.forename: Venkatram R
authors.initials: VR
authors.lastname: Mereddy
keywords: Warburg effect; colorectal adenocarcinoma; monocarboxylate transporter 1; reverse Warburg effect; α-cyano-4-hydroxycinnamic acid