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Small Molecules as Anticancer Drugs: Successes, Challenges, and Opportunities

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 October 2022) | Viewed by 2877

Special Issue Editor


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Guest Editor
Chemistry Institute, University National Autonomous of Mexico, 04510 Ciudad de México, Mexico
Interests: anticancer compounds; natural products chemistry; natural and synthetic anticancer compounds combinations

Special Issue Information

Dear Colleagues,

There was a time in which chemotherapy, a method of removing or inhibiting the growth and proliferation of tumor cells using chemical drugs, was the only approach to anticancer drug therapy. The most critical negative feature of chemotherapy is the incapacity to differentiate between cancer cells and normal cells, leading to significant toxicity and side effects. However, over the past two decades, there has been a significant paradigm shift in cancer treatment. For example, the ABL inhibitor imatinib is considered an innovative drug that validated the concept of designing a small therapeutic molecule to treat chronic myeloid leukaemia in which the malignancy is driven by translocation BCR-BL. Imatinib was the first targeted drug approved by the FDA in 2001. In the past 20 years, there has been a significant increase in targeted drugs approved by the FDA to treat cancer. On the other hand, the drug reuse technique has become an effective alternative strategy to discover and develop new cancer drug candidates. Likewise, the identification and validation of biomarkers and drug targets associated with cancer progression present an exciting opportunity to improve the treatment of this overwhelming disease.

Dr. Mariano Martínez-Vázquez
Guest Editor

Manuscript Submission Information

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Keywords

  • anti-cancer natural products
  • anti-tumoral synthetic compounds
  • anti-tumoral nanoparticles
  • small-molecule targeted drugs
  • drug repurposing

Published Papers (1 paper)

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Research

11 pages, 2065 KiB  
Article
Anti-Cancer Activity of Buthus occitanus Venom on Hepatocellular Carcinoma in 3D Cell Culture
by Ayoub Lafnoune, Su-Yeon Lee, Jin-Yeong Heo, Khadija Daoudi, Bouchra Darkaoui, Salma Chakir, Rachida Cadi, Khadija Mounaji, David Shum, Haeng-Ran Seo and Naoual Oukkache
Molecules 2022, 27(7), 2219; https://doi.org/10.3390/molecules27072219 - 29 Mar 2022
Cited by 3 | Viewed by 2390
Abstract
Hepatocellular carcinoma (HCC) is the most dominant primary liver cancer, which can be caused by chronic hepatitis virus infections and other environmental factors. Resection, liver transplantation, and local ablation are only a few of the highly effective and curative procedures presently accessible. However, [...] Read more.
Hepatocellular carcinoma (HCC) is the most dominant primary liver cancer, which can be caused by chronic hepatitis virus infections and other environmental factors. Resection, liver transplantation, and local ablation are only a few of the highly effective and curative procedures presently accessible. However, other complementary treatments can reduce cancer treatment side effects. In this present work, we evaluated the activity of Moroccan scorpion venom Buthus occitanus and its fractions obtained by chromatography gel filtration against HCC cells using a 3D cell culture model. The venom was fractionated by gel filtration chromatography, each fraction and the crude venom was tested on normal hepatocytes (Fa2N-4 cells). Additionally, the fractions and the crude venom were tested on MCTSs (multicellular tumor spheroids), and this latter was generated by cultivate Huh7.5 cancer cell line with WI38 cells, LX2 cells, and human endothelial cells (HUVEC). Our results indicate that Buthus occitanus venom toxin has no cytotoxic effects on normal hepatocytes. Moreover, it is reported that F3 fraction could significantly inhibit the MCTS cells. Other Protein Separation Techniques (High-performance liquid chromatography) are needed in order to identify the most active molecule. Full article
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