Multi-Targeting Anticancer Agents: Rational Approaches, Synthetic Routes and Structure Activity Relationship

Area of Science:

• Oncology
• Medicinal Chemistry
• Pharmacology

Background:

• Complex diseases, such as cancer, involve multiple pathogenic mechanisms, challenging traditional single-compound, single-target therapeutic approaches.
• The limitations of one-compound, one-target strategies necessitate the exploration of more sophisticated therapeutic paradigms.

Purpose of the Study:

• To review emerging strategies in anti-cancer drug discovery focusing on the one-compound-various-targets approach.
• To discuss six types of dual targeting agents, their design, synthesis, and pharmacological properties.

Main Methods:

• Literature review of dual targeting agents in anti-cancer drug discovery.
• Analysis of design and synthesis strategies for multi-targeted agents.
• Examination of pharmacological profiles and molecular interactions of dual inhibitors.

Main Results:

• Identification and discussion of six distinct categories of dual targeting agents.
• Elucidation of various molecular interactions underlying the efficacy of these agents.
• Overview of current trends and innovative strategies in dual inhibitor development.

Conclusions:

• Simultaneous targeting of multiple pathways offers enhanced therapeutic efficacy compared to single-target therapies.
• Dual targeting agents represent a promising strategy for developing next-generation anti-cancer drugs.
• This review provides valuable insights for researchers designing novel multi-targeted anti-cancer therapeutics.