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 Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor, published in 2020-03-26, which mentions a compound: 3395-91-3, mainly applied to harmine derivative preparation DYRK1A inhibitory activity diabetes SAR, Category: benzothiophene.
Recently, our group identified that harmine is able to induce β-cell proliferation both in vitro and in vivo, mediated via the DYRK1A-NFAT pathway. Since, harmine suffers from a lack of selectivity, both against other kinases and CNS off-targets, we therefore sought to expand structure-activity relationships for harmine’s DYRK1A activity, to enhance selectivity for off-targets while retaining human β-cell proliferation activity. We carried out optimization of the 9-N-position of harmine to synthesize 29 harmine-based analogs. Several novel inhibitors showed excellent DYRK1A inhibition and human β-cell proliferation capability. An optimized DYRK1A inhibitor, compound I, was identified as a novel, efficacious in vivo lead candidate. Compound I also demonstrates improved selectivity for kinases and CNS off-targets, as well as in vivo efficacy for β-cell proliferation and regeneration at lower doses than harmine. Collectively, these findings demonstrate that compound I is a much improved in vivo lead candidate as compared to harmine for the treatment of diabetes.
After consulting a lot of data, we found that this compound(3395-91-3)Category: benzothiophene can be used in many types of reactions. And in most cases, this compound has more advantages.
Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem