Cancer remains one of the unsolved diseases of today’s advanced drug discovery world
even though it is known to humans for centuries. There is continued effort to discover new
chemotherapeutic agents to improve the outcome of cancer patients. Small-molecule agonists at tolllike
receptor 7 and 8 (TLR7/8) have recently generated renewed interest in cancer research owing to
their profound antitumoral activity. TLR-7/8 agonist imidazoquinolines (Imiquimod, and Resiquimod) and dual inhibitor
of phosphoinositide 3-kinase and mammalian target of rapamycin (NVP-BEZ235) have emerged as clinically important
candidates for treating cancers. This article reviews briefly the synthesis, structure-activity relationship (SAR) and
biological activities of clinically studied imidazoquinolines along with novel emerging preclinical imidazoquinolines for
the anticancer activity.
Keywords: Anticancer agent, imidazoquinolines, imiquimod, toll-like receptor, structure-activity relationship.
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