Boron-based hybrids as novel scaffolds for the development of drugs with neuroprotective properties

Cacciatore I., TÜRKEZ H. , Di Rienzo A., Ciulla M., Mardinoglu A., Di Stefano A.

RSC MEDICINAL CHEMISTRY, 2021 (Journal Indexed in SCI) identifier

  • Publication Type: Article / Article
  • Publication Date: 2021
  • Doi Number: 10.1039/d1md00177a
  • Title of Journal : RSC MEDICINAL CHEMISTRY


Novel boron-based compounds (BBCs) were synthesized and evaluated as potential candidates for the development of novel drugs against Alzheimer's disease (AD). The neuroprotective profile of novel BBCs was evaluated using A beta 1-42-treated-SH-SY5Y cells while their antioxidant activity was evaluated by total antioxidant capacity (TAC) and total oxidative status (TOS) assays. Results showed that BLA (a novel boron-based hybrid containing an antioxidant portion) inhibited cell death induced by A beta 1-42-exposure in differentiated SH-SY5Y cells, resulting in an increase in cell viability by 25-33% (MTT assay) and by 63-71% (LDH assay) in a concentration range of 25-100 mu M. Antioxidant assays demonstrated a good capability of BLA to counteract the oxidative status. Moreover, BLA possessed a significant ability to inhibit acetylcholinesterase (AChE) (22.96% at 50 mu M), an enzyme whose enzymatic activity is increased in AD patients. In the present work, absorption and distribution properties of boron-based hybrids were predicted using Pre-ADMET software. In vitro preliminary results suggested that boron-based hybrids could be new structural scaffolds for the development of novel drugs for the management of AD.