Advancements in Synthetic Small Molecules as Anti-cancer Therapeutics

A special issue of Biomedicines (ISSN 2227-9059). This special issue belongs to the section "Cancer Biology and Oncology".

Deadline for manuscript submissions: 30 June 2024 | Viewed by 608

Special Issue Editors


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Guest Editor
Department of Pharmacology, College of Medicine, Penn State University, Hershey, PA 17033, USA
Interests: medicinal chemistry; organic synthesis; pharmacology; drug discovery; molecular docking; anti-cancer activities
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Co-Guest Editor
Department of Biologcial Sciences, University of Toledo, Toledo, OH 43606, USA
Interests: design, synthesis, and biological evaluation of small molecule inhibitors targeting various enzymes and proteins

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Co-Guest Editor
Department of Chemistry, Washington State University, Pullman, WA 99164, USA
Interests: organic synthesis; drug discovery; medicinal chemistry; nano medicine; macromolecular chemistry

Special Issue Information

Dear Colleagues,

Cancer is the uncontrolled, rapid, and pathological proliferation of abnormal cells, which is a tremendous problem worldwide today. According to the World Health Organization (WHO), cancer is the second leading cause of death globally. Its treatment remains challenging for the scientific community. One major problem with its treatment is that most of the currently available drugs are unable to differentiate between normal and abnormal cells, which is the reason behind their side effects such as thrombocytopenia, anemia, delirium, edema, etc. Drug resistance is also an issue with the current treatment of cancer. Anticancer therapeutics refer to treatments or drugs that are used to combat cancer. Anticancer small molecules, also known as small molecule inhibitors, are a type of therapeutic agent used in cancer treatment. These molecules are small organic compounds that can penetrate cells and interact with specific targets involved in cancer cell growth and survival. They work by inhibiting or interfering with the activity of proteins or pathways that are essential for cancer cell proliferation. These molecules have advantages in some aspects, such as pharmacokinetic (PK) properties, costs, patient compliance, and drug storage and transportation. This Special Issue welcomes research and up-to-date review articles addressing current research on anticancer therapeutics, with a particular focus on discovering novel anti-cancer small molecules.

Dr. Amandeep Singh
Guest Editor

Dr. Harbinder Singh
Dr. Anu Rani
Co-Guest Editors

Manuscript Submission Information

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Keywords

  • anticancer therapeutics
  • cancer targeting
  • small molecules
  • drug resistance

Published Papers (1 paper)

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Review

41 pages, 1738 KiB  
Review
Coumarin as an Elite Scaffold in Anti-Breast Cancer Drug Development: Design Strategies, Mechanistic Insights, and Structure–Activity Relationships
by Atamjit Singh, Karanvir Singh, Kamaljit Kaur, Amandeep Singh, Aman Sharma, Kirandeep Kaur, Jaskirat Kaur, Gurleen Kaur, Uttam Kaur, Harsimran Kaur, Prabhsimran Singh and Preet Mohinder Singh Bedi
Biomedicines 2024, 12(6), 1192; https://doi.org/10.3390/biomedicines12061192 - 27 May 2024
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Abstract
Breast cancer is the most common cancer among women. Currently, it poses a significant threat to the healthcare system due to the emerging resistance and toxicity of available drug candidates in clinical practice, thus generating an urgent need for the development of new [...] Read more.
Breast cancer is the most common cancer among women. Currently, it poses a significant threat to the healthcare system due to the emerging resistance and toxicity of available drug candidates in clinical practice, thus generating an urgent need for the development of new potent and safer anti-breast cancer drug candidates. Coumarin (chromone-2-one) is an elite ring system widely distributed among natural products and possesses a broad range of pharmacological properties. The unique distribution and pharmacological efficacy of coumarins attract natural product hunters, resulting in the identification of numerous natural coumarins from different natural sources in the last three decades, especially those with anti-breast cancer properties. Inspired by this, numerous synthetic derivatives based on coumarins have been developed by medicinal chemists all around the globe, showing promising anti-breast cancer efficacy. This review is primarily focused on the development of coumarin-inspired anti-breast cancer agents in the last three decades, especially highlighting design strategies, mechanistic insights, and their structure–activity relationship. Natural coumarins having anti-breast cancer efficacy are also briefly highlighted. This review will act as a guideline for researchers and medicinal chemists in designing optimum coumarin-based potent and safer anti-breast cancer agents. Full article
(This article belongs to the Special Issue Advancements in Synthetic Small Molecules as Anti-cancer Therapeutics)
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