Design, synthesis, and evaluation of bioactive small molecules

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Translational Research

Background:

• Organic chemistry is crucial for drug discovery, enabling the synthesis of diverse small molecules for screening.
• Translational research focuses on developing treatments for major diseases like Alzheimer's disease (AD), breast cancer, and viral infections.

Purpose of the Study:

• To discover lead compounds for AD, breast cancer, and viral infections using advanced organic synthesis.
• To explore novel therapeutic strategies targeting neurodegeneration, cancer proliferation, and viral replication.

Main Methods:

• Rational design and synthesis of tricyclic pyrone (TP) compounds for AD.
• Development of substituted quinoline-based gap-junction enhancers for breast cancer.
• Synthesis of novel antiviral inhibitors against resistant and understudied viruses.

Main Results:

• TP compounds preserved memory and motor functions in AD mouse models, potentially by inhibiting amyloid-beta (Aβ) aggregation and enhancing neuronal function.
• Substituted quinolines demonstrated potent in vitro and in vivo inhibitory activity against breast cancer cells.
• Ongoing research into new antiviral agents addresses the need for alternatives to existing drugs facing resistance.

Conclusions:

• The synthesized compounds show potential as drug candidates for Alzheimer's disease, breast cancer, and viral infections.
• This research highlights the power of organic synthesis in addressing critical unmet medical needs.
• Further development of these compounds could lead to novel therapeutic interventions for these diseases.