In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Synthesis and anticancer activity of novel Actinonin derivatives as HsPDF inhibitors, published in 2020-07-09, which mentions a compound: 591-54-8, mainly applied to peptidomimetic actinonin peptide synthesis antitumor structure activity HsPDF inhibitor; acyl chloride coupling chiral auxiliary alkylation bromoacetate oxidative hydrolysis; aromatic amine coupling proline nucleophilic addition nitrile hydroxylamine cyclization; amide amine peptide coupling hydrolysis Suzuki coupling mol docking; drug design target mechanism action, Related Products of 591-54-8.
Human mitochondrial peptide deformylase (HsPDF) is responsible for removing the formyl group from N-terminal formylmethionines of newly synthesized mitochondrial proteins and plays important roles in maintaining mitochondria function. It is overexpressed in various cancers and has been proposed as a novel therapeutic target. Actinonin, a naturally occurring peptidomimetic HsPDF inhibitor, was reported to inhibit the proliferation of a broad spectrum of human cancer cells in vitro. However, its efficacy and pharmacokinetic profile requires significant improvement for therapeutic purposes. To obtain HsPDF inhibitors as anticancer therapeutics, we screened an inhouse collection of actinonin derivatives and found two initial hits with antiproliferation activity. Further optimization along the peptidomimetic backbone lead to two series of compounds containing substituted Ph moieties. They are potent HsPDF inhibitors and exhibited greatly improved antiproliferation activity in selected cancer cell lines. Finally, compound (I) significantly inhibited the growth of human colon cancer in xenograft animal models.
Although many compounds look similar to this compound(591-54-8)Related Products of 591-54-8, numerous studies have shown that this compound(SMILES:C1=CN=CN=C1N), has unique advantages. If you want to know more about similar compounds, you can read my other articles.