Anticancer efficacy triggered by synergistically modulating the homeostasis of anions and iron: Design, synthesis and biological evaluation of dual-functional squaramide-hydroxamic acid conjugates.

Targeting the homeostasis of anions and iron has emerged as a promising therapeutic approach for the treatment of cancers. However, single-targeted agents often fall short of achieving optimal treatment efficacy. Herein we designed and synthesized a series of novel dual-functional squaramide-hydroxamic acid conjugates that are capable of synergistically modulating the homeostasis of anions and iron.

Synthesis and mechanism of biological action of morpholinyl-bearing arylsquaramides as small-molecule lysosomal pH modulators.

Lysosomal pH is an important modulator for many cellular processes. An agent that is capable of regulating lysosomal pH may find a wide range of potential applications in the field of biomedicine. In this study, we describe the synthesis of a family of morpholinyl-bearing arylsquaramides as small-molecule lysosomal pH modulators.