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Special Issue "Sulfonamides as a Potent Anti-Cancer Agents"

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Oncology".

Deadline for manuscript submissions: closed (30 April 2022) | Viewed by 1304

Special Issue Editors

Prof. Dr. Michal Szostak
E-Mail Website
Guest Editor
Department of Chemistry, Rutgers University, 73 Warren St, Newark, NJ 07102, USA
Interests: amide bonds; N-heterocyclic carbenes; C-N activation; C-H activation; C-O activation; lanthanides; cross-coupling; catalysis; reductions; reductive couplings; radical chemistry; synthetic methodology; natural products
Special Issues, Collections and Topics in MDPI journals
Dr. Katarzyna Kotwica-Mojzych
E-Mail Website
Guest Editor
Chair and Department of Histology, Embryology and Cytophysiology, Medical University of Lublin, 20-080 Lublin, Poland
Interests: design and preparation of biologically active compounds
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Mariusz Mojzych
E-Mail Website
Guest Editor
Department of Chemistry, Siedlce University of Natural Sciences and Humanities, 08-110 Siedlce, Poland
Interests: medicinal chemistry; medicinal and pharmaceutical chemistry; synthetic organic chemistry; heterocyclic chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Neoplastic diseases are one of the most important challenges of modern medical and chemical sciences due to their high frequency of occurrence and low chance for the successful recovery. Among the many methods of cancer treatment, chemotherapy plays a special role. However, the inadequacy and many side effects of the currently used chemotherapy justify the need for the continued search for new, more effective and safe cytostatics. At the same time, it should be noted that a large body of recent literature show that sulfonamides may serve as valuable leads for new and effective anti-cancer drugs with low toxicity on normal cells. This Special Issue aims to provide a broad survey of recent advances in the synthesis of sulfonamides with anticancer properties and their mechanisms of action on cancer cells. This Special Issue will contain contributions describing various aspects of this area. Reviews articles by experts in the field are also welcome.

Prof. Dr. Michal Szostak
Dr. Katarzyna Kotwica-Mojzych
Prof. Dr. Mariusz Mojzych
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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

  • sulfonamides
  • anticancer activity
  • cancer cell lines
  • apoptosis
  • cancer
  • sulfonylated derivatives
  • anticancer drugs
  • anticancer sulfonamides

Published Papers (2 papers)

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Research

Article
Preparation of Novel Pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine Sulfonamides and Their Experimental and Computational Biological Studies
Int. J. Mol. Sci. 2022, 23(11), 5892; https://doi.org/10.3390/ijms23115892 - 24 May 2022
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Abstract
Pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine sulfonamides constitute a novel class of heterocyclic compounds with broad biological activity, including anticancer properties. Investigated in this study, MM-compounds (MM134, MM136, MM137, and MM139) exhibited cytotoxic and proapoptotic activity against cancer cell [...] Read more.
Pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine sulfonamides constitute a novel class of heterocyclic compounds with broad biological activity, including anticancer properties. Investigated in this study, MM-compounds (MM134, MM136, MM137, and MM139) exhibited cytotoxic and proapoptotic activity against cancer cell lines (BxPC-3, PC-3, and HCT-116) in nanomolar concentrations without causing cytotoxicity in normal cells (L929 and WI38). In silico predictions indicate that tested compounds exhibit favorable pharmacokinetic profiles and may exert anticancer activity through the inhibition of BTK kinase, the AKT-mTOR pathway and PD1-PD-L1 interaction. Our findings point out that these sulfonamide derivatives may constitute a source of new anticancer drugs after optimization. Full article
(This article belongs to the Special Issue Sulfonamides as a Potent Anti-Cancer Agents)
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Article
Cytotoxicity of Newly Synthesized Quinazoline–Sulfonamide Derivatives in Human Leukemia Cell Lines and Their Effect on Hematopoiesis in Zebrafish Embryos
Int. J. Mol. Sci. 2022, 23(9), 4720; https://doi.org/10.3390/ijms23094720 - 25 Apr 2022
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Abstract
Many quinazoline derivatives with pharmacological properties, such as anticancer activity, have been synthesized. Fourteen quinazoline derivatives bearing a substituted sulfonamide moiety (4a–n) were previously synthesized and fully characterized. These compounds exerted antiproliferative activity against cell lines derived from solid tumors. Herein, [...] Read more.
Many quinazoline derivatives with pharmacological properties, such as anticancer activity, have been synthesized. Fourteen quinazoline derivatives bearing a substituted sulfonamide moiety (4a–n) were previously synthesized and fully characterized. These compounds exerted antiproliferative activity against cell lines derived from solid tumors. Herein, the antileukemic activities of these compounds (4a–n) against two different leukemia cell lines (Jurkat acute T cell and THP-1 acute monocytic) were investigated. Our investigation included examining their activity in vivo in a zebrafish embryo model. Remarkably, compounds 4a and 4d were the most potent in suppressing cell proliferation, with an IC50 value range of 4–6.5 µM. Flow cytometry analysis indicated that both compounds halted cell progression at the G2/M phase and induced apoptosis in a dose-dependent manner. RT-PCR and Western blot analyses also showed that both compounds effectively induced apoptosis by upregulating the expression of proapoptotic factors while downregulating that of antiapoptotic factors. In vivo animal toxicity assays performed in zebrafish embryos indicated that compound 4d was more toxic than compound 4a, with compound 4d inducing multiple levels of teratogenic phenotypes in zebrafish embryos at a sublethal concentration. Moreover, both compounds perturbed the hematopoiesis process in developing zebrafish embryos. Collectively, our data suggest that compounds 4a and 4d have the potential to be used as antileukemic agents. Full article
(This article belongs to the Special Issue Sulfonamides as a Potent Anti-Cancer Agents)
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