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Pharmaceutics
Special Issues
Promising Small Molecule Compounds in Cancer Treatment
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Promising Small Molecule Compounds in Cancer Treatment

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: closed (10 August 2024) | Viewed by 4904

Special Issue Editors

Dr. Elwira Chrobak

E-Mail Website
Guest Editor
Department of Organic Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Katowice, 4 Jagiellońska Str., 41-200 Sosnowiec, Poland
Interests: medicinal chemistry; natural products; triterpenes; organic synthesis; anticancer agents
Dr. Ewa Bębenek

E-Mail Website
Guest Editor
Department of Organic Chemistry, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia in Katowice, 4 Jagiellońska Str., 41-200 Sosnowiec, Poland
Interests: medicinal chemistry; natural products; triterpenes; organic synthesis; anticancer agents

Special Issue Information

Dear Colleagues,

We are pleased to invite you to submit original scientific articles, review papers, or communications for a Special Issue of Pharmaceutics devoted to researching new small-molecule substances with anticancer activity.

The basis of cancer chemotherapy involves small-molecule cytostatics. These compounds are characterized by their ability to freely penetrate the lipid bilayer, and their solubility in water allows them to move around the body. Currently used cytostatics do not work selectively and also cause damage to normal cells. Their low selectivity and narrow therapeutic index determine high toxicity and lead to numerous side effects. Actions are constantly needed to improve the therapeutic index of the cytostatics used, inter alia, by interfering with the chemical structure of drugs. Research is also being conducted for new and developing derivatives with better pharmacokinetic properties and preparations, including the slow release of active substances.

This Special Issue aims to present the latest reports on natural and synthetic small-molecule compounds with anticancer activity, their preparation, the determination of the pharmacokinetic profile, and in vitro and in vivo studies.

Dr. Elwira Chrobak
Dr. Ewa Bębenek
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • anticancer agents
  • natural products
  • synthesis
  • structure modification
  • structure–activity relationship
  • substance action on target
  • biological evaluation
  • cancer therapy

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (2 papers)

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Review

39 pages, 12757 KiB  
Review
Biological Evaluations and Computer-Aided Approaches of Janus Kinases 2 and 3 Inhibitors for Cancer Treatment: A Review
by Lenci K. Vázquez-Jiménez, Gildardo Rivera, Alfredo Juárez-Saldivar, Jessica L. Ortega-Balleza, Eyra Ortiz-Pérez, Elena Jaime-Sánchez, Alma Paz-González and Edgar E. Lara-Ramírez
Pharmaceutics 2024, 16(9), 1165; https://doi.org/10.3390/pharmaceutics16091165 - 4 Sep 2024
Cited by 1 | Viewed by 1516
Abstract
Cancer remains one of the leading diseases of mortality worldwide. Janus kinases 2/3 (JAK2/3) have been considered a drug target for the development of drugs to treat different types of cancer. JAK2/3 play a critical role in innate immunity, inflammation, and hematopoiesis by [...] Read more.
Cancer remains one of the leading diseases of mortality worldwide. Janus kinases 2/3 (JAK2/3) have been considered a drug target for the development of drugs to treat different types of cancer. JAK2/3 play a critical role in innate immunity, inflammation, and hematopoiesis by mediating the signaling of numerous cytokines, growth factors, and interferons. The current focus is to develop new selective inhibitors for each JAK type. In this review, the current strategies of computer-aided studies, and biological evaluations against JAK2/3 are addressed. We found that the new synthesized JAK2/3 inhibitors are prone to containing heterocyclic aromatic rings such as pyrimidine, pyridine, and pyrazolo [3,4-d]pyrimidine. Moreover, inhibitors of natural origin derived from plant extracts and insects have shown suitable inhibitory capacities. Computer-assisted studies have shown the important features of inhibitors for JAK2/3 binding. Biological evaluations showed that the inhibition of the JAK receptor affects its related signaling pathway. Although the reviewed compounds showed good inhibitory capacity in vitro and in vivo, more in-depth studies are needed to advance toward full approval of cancer treatments in humans. Full article
(This article belongs to the Special Issue Promising Small Molecule Compounds in Cancer Treatment)
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30 pages, 6548 KiB  
Review
Synthesis, Pharmacological Properties, and Potential Molecular Mechanisms of Antitumor Activity of Betulin and Its Derivatives in Gastrointestinal Cancers
by Marcel Madej, Joanna Gola and Elwira Chrobak
Pharmaceutics 2023, 15(12), 2768; https://doi.org/10.3390/pharmaceutics15122768 - 13 Dec 2023
Cited by 5 | Viewed by 2346
Abstract
Gastrointestinal (GI) cancers are an increasingly common type of malignancy, caused by the unhealthy lifestyles of people worldwide. Limited methods of treatment have prompted the search for new compounds with antitumor activity, in which betulin (BE) is leading the way. BE as a [...] Read more.
Gastrointestinal (GI) cancers are an increasingly common type of malignancy, caused by the unhealthy lifestyles of people worldwide. Limited methods of treatment have prompted the search for new compounds with antitumor activity, in which betulin (BE) is leading the way. BE as a compound is classified as a pentacyclic triterpene of the lupane type, having three highly reactive moieties in its structure. Its mechanism of action is based on the inhibition of key components of signaling pathways associated with proliferation, migration, interleukins, and others. BE also has a number of biological properties, i.e., anti-inflammatory, hepatoprotective, neuroprotective, as well as antitumor. Due to its poor bioavailability, betulin is subjected to chemical modifications, obtaining derivatives with proven enhanced pharmacological and pharmacokinetic properties as a result. The method of synthesis and substituents significantly influence the effect on cells and GI cancers. Moreover, the cytotoxic effect is highly dependent on the derivative as well as the individual cell line. The aim of this study is to review the methods of synthesis of BE and its derivatives, as well as its pharmacological properties and molecular mechanisms of action in colorectal cancer, hepatocellular carcinoma, gastric cancer, and esophageal cancer neoplasms. Full article
(This article belongs to the Special Issue Promising Small Molecule Compounds in Cancer Treatment)
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