具有PARP-1抑制活性的吡嗪类化合物

maiy Jaballah, Norhan Abdelrahman, Ahmed Al-Karmalawy, Khaled Abouzid
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Pyridazine Based Compounds with PARP-1 Inhibitory Activity
Pyridazine-based compounds have been identified as potent PARP1 inhibitors. The PARP is an enzyme family essential for many cellular activities such as the Repair of DNA, apoptosis, and genomic stability, also known as poly (ADP-ribose) synthetases and poly (ADP-ribose) transferases. PARP1 (Poly (ADP-ribose) polymerase 1) is an enzyme that plays a critical role in DNA repair and maintenance of genomic stability. The inhibition of PARP1 has emerged as a promising strategy for the treatment of various cancers, especially those with defects in DNA repair pathways. An array of Diazine-based-containing compounds was recognized as redoubtable PARP1 inhibitors, including Olaparib, and Talazoparib. These compounds have manifested successful results in clinical studies, exhibiting their benefit in various cancer therapies, including ovarian, breast, and pancreatic cancers. In the following review, we will highlight some of the most recent Pyridazine-based compounds and their role in the development of tacit PAPR1 inhibitors.
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