Synthesis and Biological Evaluation of Marine-Inspired Benzothiazole Derivatives as Retinoid X Receptor-α Antagonists with Anti-Cancer Activities.

ABSTRACT: Retinoid X receptor α (RXRα) plays a vital role in multiple biological and pathological processes and represents a promising therapeutic target for anti-tumor drug design. Inspired by the marine-derived RXRα antagonist meroterpenthiazole A, 21 undescribed benzothiazole derivatives were designed and synthesized. The inhibitory effects of 21 derivatives on RXRα transactivation and their anti-tumor activities against MDA-MB-231 cells were evaluated. Compounds 4a-4h, 6a-6b, 7c-7f, and 7h-7i inhibited 9-cis-retinoic acid-induced RXRα transactivation, while compounds 3b, 4f-4h, 7a, 7c, 7f, and 7h-7i exhibited inhibitory effects on the proliferation of MDA-MB-231 cells. Meanwhile

SUBMITTER: Lin Y 

PROVIDER: S-EPMC12471517 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature