Abstract: The present invention generally relates to the field of transporter modulators, e.g., monocarboxylate transporter inhibitors, and more particularly to new bicyclic enone carboxylate compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with monocarboxylate transporter activity such as in treating cancer and other neoplastic disorders, tissue and organ transplant rejection.

Abstract: The present disclosure provides a method of treating cancer in a subject. The method including administering to the subject: a) a therapeutically effective amount of a monocarboxylate transporter (MCT) inhibitor alone; or in combination with b) a therapeutically effective amount of an immunotherapy agent, wherein the monocarboxylate transporter inhibitor is represent by Formula (I): or a pharmaceutically acceptable salt thereof, wherein subscript n, B, W, X, Y, Z, each A, each R1, and R2 are as provided herein. Also provided are a pharmaceutical composition thereof and a kit thereof for treating cancer in a subject.