Li, Shuai; Li, Xin-yang; Zhang, Ting-jian; Zhu, Ju; Liu, Kai-li; Wang, De-pu; Meng, Fan-hao published their research in Bioorganic Chemistry in 2021. The article was titled 《Novel 4,5-dihydrospiro[benzo[c]azepine-1,1′-cyclohexan]-3(2H)-one derivatives as PARP-1 inhibitors: Design, synthesis and biological evaluation》.Reference of 2-Hydroxyphenylboronic acid The article contains the following contents:
To further explore the research of novel PARP-1 inhibitors, design and synthesis of a series of novel 4,5-dihydrospiro[benzo[c]azepine-1,1′-cyclohexan]-3(2H)-one derivatives I (R = H, 2-Cl, 3-F, etc.) PARP-1 inhibitors based on the author’s previous research is reported. Most compounds displayed certain antitumor activities against four tumor cell lines (A549, HepG2, HCT-116, and MCF-7). Specifically, the candidate compound I (R = 2-F) possessed strong anti-proliferative potency toward A549 cells with the IC50 value of 2.01μM and showed low toxicity to lung cancer cell line. And the in vitro enzyme inhibitory activity of compound I (R = 2-F) was better than rucaparib. Mol. docking studies provided a rational binding model of the above compound in complex with rucaparib. The following cell cycle and apoptosis assays revealed that this compound could arrest cell cycle in the S phase and induce cell apoptosis and western blot anal. further showed that it could effectively inhibit the PAR’s biosynthesis and was more effective than rucaparib. Overall, based on the biol. activity evaluation, compound I (R = 2-F) could be a potential lead compound for further developing novel amide PARP-1 inhibitors. In the experiment, the researchers used 2-Hydroxyphenylboronic acid(cas: 89466-08-0Reference of 2-Hydroxyphenylboronic acid)
2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Reference of 2-Hydroxyphenylboronic acid
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