Our group focuses on the efficient synthesis of bioactive natural products by deeply integrating chemistry and biology, and on investigating their bioactivities to accelerate the discovery of novel lead compounds. We aim to develop new chemical and chemoenzymatic strategies that provide facile access to underexplored chemical space, thereby facilitating biological evaluation, target identification, and mechanistic elucidation. Ultimately, these studies would allow us to identify bioactive small molecules with transcriptional regulatory activity and to generate molecular probes for elucidating nuclear receptor-mediated transcriptional regulatory mechanisms.