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Anticancer Agents Med Chem. 2019;19(7):842-874. doi: 10.2174/1871520619666190118120708.

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

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Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab-143005, India.
Program in Chemical Biology, Sloan Kettering Institute, New York, NY 10065, United States.


We live in a world with complex diseases such as cancer which cannot be cured with one-compound one-target based therapeutic paradigm. This could be due to the involvement of multiple pathogenic mechanisms. One-compound-various-targets stratagem has become a prevailing research topic in anti-cancer drug discovery. The simultaneous interruption of two or more targets has improved the therapeutic efficacy as compared to the specific targeted based therapy. In this review, six types of dual targeting agents along with some interesting strategies used for their design and synthesis are discussed. Their pharmacology with various types of the molecular interactions within their specific targets has also been described. This assemblage will reveal the recent trends and insights in front of the scientific community working in dual inhibitors and help them in designing the next generation of multi-targeted anti-cancer agents.


Histone deacetylase; anticancer; heat shock protein; kinase; topoisomerase; tubulin.

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