Figure 1.
Structures of PT2385 and MK-6482 (also known as PT2977), specific inhibitors of HIF-2α. Structure of the originally designed HIF-2α inhibitor PT2385, which contains the difluoro group in the geminal position, was modified to enhance the pharmacokinetics and efficacy of MK-6482 in which the difluoro group is in the vicinal position.53