Monocarboxylate transporter 1 inhibitors as potential anticancer agents

Shirisha Gurrapu; Sravan K. Jonnalagadda; Mohammad A. Alam; Grady L. Nelson; Mary G. Sneve; Lester R Drewes; Venkatram R Mereddy

doi:10.1021/acsmedchemlett.5b00049

Monocarboxylate transporter 1 inhibitors as potential anticancer agents

Shirisha Gurrapu, Sravan K. Jonnalagadda, Mohammad A. Alam, Grady L. Nelson, Mary G. Sneve, Lester R Drewes, Venkatram R Mereddy

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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.

Original language	English (US)
Pages (from-to)	558-561
Number of pages	4
Journal	ACS Medicinal Chemistry Letters
Volume	6
Issue number	5
DOIs	https://doi.org/10.1021/acsmedchemlett.5b00049
State	Published - May 14 2015

Bibliographical note

Publisher Copyright:
© 2015 American Chemical Society.

Keywords

Warburg effect
colorectal adenocarcinoma
monocarboxylate transporter 1
reverse Warburg effect
α-cyano-4-hydroxycinnamic acid

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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.",

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AU - Jonnalagadda, Sravan K.

AU - Alam, Mohammad A.

AU - Nelson, Grady L.

AU - Sneve, Mary G.

AU - Drewes, Lester R

AU - Mereddy, Venkatram R

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Monocarboxylate transporter 1 inhibitors as potential anticancer agents

Abstract

Bibliographical note

Keywords

UN SDGs

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