Antarlides are a family of macrocyclic polyketide natural products (antarlides A–H) isolated from Streptomyces sp. BB47.^[1][2] These compounds are notable for their potent activity as androgen receptor (AR) antagonists, including activity against mutant ARs associated with resistance to clinically used antiandrogens.^[1]

Antarlides act as androgen receptor antagonists, inhibiting both wild-type and clinically relevant mutant ARs in vitro. This activity is significant for the treatment of prostate cancer, particularly in cases where resistance to standard AR antagonists has developed.^[1]

The complex structure of antarlides has inspired synthetic efforts. A recent report describes a practical and efficient synthesis of the C8–C23 fragment of antarlides A–H, incorporating six stereocenters and a conjugated diene. This synthesis utilized CBS reduction, Evans' aldol reaction, Keck–Maruoka allylation, and enzymatic resolution, demonstrating the feasibility of assembling key structural motifs of the antarlides.^[3]