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Novel Anticancer Compounds
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Novel Anticancer Compounds

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

Deadline for manuscript submissions: closed (1 November 2021) | Viewed by 3739

Special Issue Editors

Prof. Dr. Francesco Leonetti

E-Mail Website
Guest Editor
Università degli Studi di Bari, Bari, Italy
Interests: P-glycoprotein; cancer
Dr. Angela Stefanachi

E-Mail Website
Guest Editor
Department of Pharmacy-Drug Sciences, University of Bari, 70125 Bari, Italy
Interests: BCR-ABL inhibitors; HDAC inhibitors; CB2 modulators
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The development of new anticancer compounds is a challenging goal for a medicinal chemist because of the complexity of this pathology. It is fundamental to understand the mechanisms involved in cancer growth and progression, together with resistance phenomena and cytotoxicity concerns, before starting a novel anticancer compound design. Anticancer drug development, indeed, requires a total vision of the complete pathology process.Numerous strategies have been used to achieve this goal and they include the development of tyrosine kinases inhibitors, monoclonal antibodies, antibody drug conjugates (ADC), antisense and siRNA. The multitarget directed ligands approach must also be remembered, because it was shown to be very useful in multifactorial pathology such as cancer.This issue will collect contributions from researchers working on anticancer compounds development in different areas, including molecular modeling, chemical synthesis, drug delivery, molecular biology and pharmacology. Original studies, reviews, opinion papers, or short communications are welcome. 

Prof. Dr. Francesco Leonetti
Dr. Angela Stefanachi
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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 compounds
  • chemical synthesis
  • molecular modeling
  • drug delivery
  • biological screening

Published Papers (1 paper)

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Research

17 pages, 4734 KiB  
Article
Anti-Cancer Effects of Zotarolimus Combined with 5-Fluorouracil Treatment in HCT-116 Colorectal Cancer-Bearing BALB/c Nude Mice
by Geng-Ruei Chang, Chan-Yen Kuo, Ming-Yang Tsai, Wei-Li Lin, Tzu-Chun Lin, Huei-Jyuan Liao, Chung-Hung Chen and Yu-Chen Wang
Molecules 2021, 26(15), 4683; https://doi.org/10.3390/molecules26154683 - 02 Aug 2021
Cited by 13 | Viewed by 3170
Abstract
Zotarolimus is a semi-synthetic derivative of rapamycin and an inhibitor of mammalian target of rapamycin (mTOR) signaling. Currently, zotarolimus is used to prolong the survival time of organ grafts, but it is also a novel immunosuppressive agent with potent anti-proliferative activity. Here, we [...] Read more.
Zotarolimus is a semi-synthetic derivative of rapamycin and an inhibitor of mammalian target of rapamycin (mTOR) signaling. Currently, zotarolimus is used to prolong the survival time of organ grafts, but it is also a novel immunosuppressive agent with potent anti-proliferative activity. Here, we examine the anti-tumor effect of zotarolimus, alone and in combination with 5-fluorouracil, on HCT-116 colorectal adenocarcinoma cells implanted in BALB/c nude mice. Compared with the control mice, mice treated with zotarolimus or zotarolimus combined with 5-FU showed retarded tumor growth; increased tumor apoptosis through the enhanced expression of cleaved caspase 3 and extracellular signal-regulated kinase (ERK) phosphorylation; reduced inflammation-related factors such as IL-1β, TNF-α, and cyclooxygenase-2 (COX-2) protein; and inhibited metastasis-related factors such as CD44, epidermal growth factor receptor (EGFR), transforming growth factor β (TGF-β), and vascular endothelial growth factor (VEGF). Notably, mice treated with a combination of zotarolimus and 5-FU showed significantly retarded tumor growth, reduced tumor size, and increased tumor inhibition compared with mice treated with 5-FU or zotarolimus alone, indicating a strong synergistic effect. This in vivo study confirms that zotarolimus or zotarolimus combined with 5-FU can be used to retard colorectal adenocarcinoma growth and inhibit tumorigenesis. Our results suggest that zotarolimus may increase the chemo-sensitization of tumor cells. Therefore, zotarolimus alone and zotarolimus combined with 5-FU may be potential anti-tumor agents in the treatment of human colon adenocarcinoma. Future research on zotarolimus may lead to the development of new therapeutic strategies. Full article
(This article belongs to the Special Issue Novel Anticancer Compounds)
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