Abstract
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.
Mini-Reviews in Medicinal Chemistry
Title:Imidazoquinolines: Recent Developments in Anticancer Activity
Volume: 16 Issue: 4
Author(s): Shivaputra A. Patil, Siddappa A. Patil, Renukadevi Patil and Rintaro Hashizume
Affiliation:
Keywords: Anticancer agent, imidazoquinolines, imiquimod, toll-like receptor, structure-activity relationship.
Abstract: 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.
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Patil A. Shivaputra, Patil A. Siddappa, Patil Renukadevi and Hashizume Rintaro, Imidazoquinolines: Recent Developments in Anticancer Activity, Mini-Reviews in Medicinal Chemistry 2016; 16 (4) . https://dx.doi.org/10.2174/1389557516666151217122758
DOI https://dx.doi.org/10.2174/1389557516666151217122758 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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