Poly (ADP-ribose) polymerase (PARP) is a family of enzymes containing 17 members, of which 15 have been shown to catalyze the transfer ADP-ribose to target proteins[1]. PARP1 and PARP2 play important roles in DNA repair, making them an attractive target for oncology. PARP1 has been considered a new drug target based on the synthetic lethality strategy in BRCA1/2-mutated cancer patients. Currently, there are four FDA-approved PARP inhibitors in the market (Olaparib, Rucaparib, Niraparib, Talazoparib) for the treatment of recurrent ovarian cancer and breast cancer[2-7]. At the AACR annual meeting 2022, AstraZeneca disclosed the clinical trial results of AZD5305. The results show that AZD5305 is a highly selective PARP1 inhibitor with good safety and clinical activity in a variety of cancers[8-9].
A series of building blocks will be used as molecular fragments in the design of PARP inhibitors
[1] Journal of Medicinal Chemistry (2020), 63, 23, 14151-14183. [2] European Journal of Medicinal Chemistry (2020), 204, 112635. [3] Journal of Medicinal Chemistry (2020), 63, 24, 15541-15563. [4] European Journal of Medicinal Chemistry (2019), 165, 198-215. [5] Journal of Medicinal Chemistry (2015), 58, 21, 8683-8693. [6] Journal of Medicinal Chemistry (2017), 60, 4, 1262-1271. [7] Nature (2020), 579, 598-602. [8] WO2021013735A1. [9] WO2021260092A1.
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