《Synthesis and structure-activity relationship studies of LLY-507 analogues as SMYD2 inhibitors》 was written by Zhang, Bin; Liao, Liping; Wu, Fan; Zhang, Fengcai; Sun, Zhongya; Chen, Haijun; Luo, Cheng. Recommanded Product: 2-Hydroxyphenylboronic acid And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020. The article conveys some information:
SET and MYND domain-containing protein 2 (SMYD2), a lysine methyltransferase, is reported to catalyze the methylation of lysine residues on histone and non-histone proteins. As a potential target for cancer therapy, there are several SMYD2 inhibitors are reported, LLY-507 as a cell-active inhibitor exhibits submicromolar potency against SMYD2 in several cancer cell lines. To know which structural fragment of LLY-507 is suitable for chem. modification, three sites are chosen for structure-activity relationship studies (SARs). Among our focused library, compounds 43 and 44 with amide link on site C showed reasonably improved potency indicating that modification on this fragment is more flexible and introduction of electrophilic warheads in this position might provide lysine-targeting covalent inhibitors for SMYD2. The experimental part of the paper was very detailed, including the reaction process of 2-Hydroxyphenylboronic acid(cas: 89466-08-0Recommanded Product: 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. Recommanded Product: 2-Hydroxyphenylboronic acid
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