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.
Export Options
About this article
Cite this article as:
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 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Modulators of Acetylcholinesterase Activity: From Alzheimer's Disease to Anti-Cancer Drugs
Current Medicinal Chemistry Induction of Molecular Chaperones as a Therapeutic Strategy for the Polyglutamine Diseases
Current Pharmaceutical Biotechnology Src Kinase Inhibitors: An Update on Patented Compounds
Current Medicinal Chemistry Substance Abuse, HIV-1 and Hepatitis
Current HIV Research Thymoquinone Inhibits Proliferation and Migration of MDA-MB-231 Triple Negative Breast Cancer Cells by Suppressing Autophagy, Beclin-1 and LC3
Anti-Cancer Agents in Medicinal Chemistry Prevalence of Vertebral Fractures, Vascular Calcifications, and Mortality in Warfarin Treated Hemodialysis Patients
Current Vascular Pharmacology Regulation of EMT by KLF4 in Gastrointestinal Cancer
Current Cancer Drug Targets Transient Expression of Chicken Antimicrobial Peptides by Mouse Mammary Carcinoma Cells C127
Protein & Peptide Letters Roles of Laminin-332 and α6β4 Integrin in Tumor Progression
Mini-Reviews in Medicinal Chemistry Modulation of Cytotoxicity of Benzamide Riboside by Expression of NMN Adenylyltransferase
Current Medicinal Chemistry Reactive Oxygen Species in Cancer Biology and Anticancer Therapy
Current Medicinal Chemistry Vagotomy and Gastric Tumorigenesis
Current Neuropharmacology Aldose Reductase Inhibitors and Nanodelivery of Diabetic Therapeutics
Mini-Reviews in Medicinal Chemistry MicroRNA: Implications for Alzheimer Disease and other Human CNS Disorders
Current Genomics Therapeutic Targets in Triple Negative Breast Cancer - Where are we now?
Recent Patents on Anti-Cancer Drug Discovery Perspectives on Chemopreventive and Therapeutic Potential of Curcumin Analogs in Medicinal Chemistry
Mini-Reviews in Medicinal Chemistry Molecular Targets of Rheumatoid Arthritis
Inflammation & Allergy - Drug Targets (Discontinued) Water and Ion Channels: Crucial in the Initiation and Progression of Apoptosis in Central Nervous System?
Current Neuropharmacology Membrane and Soluble Forms of Endoglin in Preeclampsia
Current Molecular Medicine Assessment of Nutritional Status in Cancer – The Relationship Between Body Composition and Pharmacokinetics
Anti-Cancer Agents in Medicinal Chemistry