Synthesis of Novel Anticancer Agents, Antivirals and Small Biological Molecules

A special issue of Symmetry (ISSN 2073-8994). This special issue belongs to the section "Chemistry: Symmetry/Asymmetry".

Deadline for manuscript submissions: closed (31 August 2021) | Viewed by 3175

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Guest Editor
1. Department of Natural Sciences, Southeastern University, 1000 Longfellow Blvd., Lakeland, FL 33801, USA
2. Department of Chemistry, University of South Florida, 4202 E. Fowler Ave., Tampa, FL 33620, USA
Interests: anticancer agents; antivirals; Parkinson’s disease; organic synthesis; drug design
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Dear Colleagues,

The global development of cancer registries has led to the discovery of novel drugs that derived from various sources that are used to treat several maladies including cancers and many viral diseases. About 80% of the world’s population depends on traditional therapeutics for several diseases, including anticancer and antiviral treatments. Many of these are symmetrical therapeutics (e.g., macrolides). The grouping together of antivirals, anticancer agents, and other small biological molecules from various sources in one review is not a matter of expediency, but follows from the increasing realization of the importance of the location as the most likely source of future “leads” in both areas. The currently available cancer and antiviral therapies still have various limitations, such as multi-drug resistance, undesired off-target effects, and unpredictable efficacies. The development of novel anticancer antiviral agents and other small biological molecules continues to be imperative to combat these diseases. The emerging molecular targets and signal pathways enable the development of novel strategies for the rational design of new anticancer agents, antiviral agents, and other small biologics. Numerous well-established synthetic methods and biological screening assays have paved the way for the discovery and development of new agents. Despite the availability of drugs in each area, more effective formulations are required. Some of these new drugs will undoubtedly come from natural products screening, in combination with synthetic modification, analog production, and combinatorial chemistry. In addition, the synthesis of other small biological molecules with specific disease targets are also welcome in this Special Issue of Symmetry. Both original research and review articles focusing on the rational design, synthesis, and/or biological evaluation of various anticancer and antiviral agents (including small molecules) as potential therapeutics are welcome to be submitted for publication in this Special Issue.

Prof. Dr. Ralph Salvatore
Guest Editor

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Keywords

  • anticancer agents 
  • antiviral agents 
  • drug design 
  • synthesis 
  • small biologics

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Published Papers (1 paper)

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Research

22 pages, 8152 KiB  
Article
Regio- and Stereoselective Synthesis of a New Series of Spirooxindole Pyrrolidine Grafted Thiochromene Scaffolds as Potential Anticancer Agents
by Assem Barakat, Mohammad Shahidul Islam, M. Ali, Abdullah Mohammed Al-Majid, Saeed Alshahrani, Abdullah Saleh Alamary, Sammer Yousuf and M. Iqbal Choudhary
Symmetry 2021, 13(8), 1426; https://doi.org/10.3390/sym13081426 - 4 Aug 2021
Cited by 26 | Viewed by 2812
Abstract
A series of new spiro-heterocycles engrafted spirooxindole/pyrrolidine/thiochromene scaffolds was synthesized by the three-component 1,3-dipolar cycloaddition reactions in a fully controlled regio- and stereo-selective fashion. Condensation of several substituted isatin derivatives with L-proline generated the azomethine ylides which subsequently reacted with chalcones based thiochromene [...] Read more.
A series of new spiro-heterocycles engrafted spirooxindole/pyrrolidine/thiochromene scaffolds was synthesized by the three-component 1,3-dipolar cycloaddition reactions in a fully controlled regio- and stereo-selective fashion. Condensation of several substituted isatin derivatives with L-proline generated the azomethine ylides which subsequently reacted with chalcones based thiochromene scaffold, and finally afforded the target spiro-compounds. This simple protocol furnished a structurally complex, biologically relevant spiro-heterocycles in good yields through a one-pot process. All synthesized chalcone-based thiochromene, along with the spirooxindole/pyrrolidine/thiochromene scaffolds, were tested for their anticancer activity against four cancer cell lines (PC3, HeLa, MCF-7, and MDA-MB231). Toxicity of these compounds was also evaluated against human fibroblast BJ cell line, and they appeared to be not cytotoxic. For the prostate cancer (PC3) cell line, the most active hybrid, among synthesized series, was compound (7f, IC50 = 8.7 ± 0.7 µM). The most potent spirooxindole/pyrrolidine/thiochromene hybrid against cervical (HeLa) cancer cells was compound (7k, IC50 = 8.4 ± 0.5 µM) having chlorine and p-trifluoromethyl substituents attached to phenyl rings. Finally, against the MCF-7 and MDA-MB231 breast cancer cell lines, compound (7d) was the most active member of this series (IC50 = 7.36 ± 0.37, and 9.44 ± 0.32 µM, respectively). Full article
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