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Advances in Chemoprevention: Development of Ligands Interfering with the Carcinogenesis

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

Deadline for manuscript submissions: closed (30 November 2020) | Viewed by 3126

Special Issue Editors


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Guest Editor
Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, TX 79106, USA
Interests: drug discovery; medicinal chemistry and chemical biology in the areas of neurodegenerative disorders; cancer and microbiology

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Guest Editor
Department of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, Jerry H. Hodge School of Pharmacy, Amarillo, TX, USA
Interests: Vascular biology, angiogenesis, tumor metastasis
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
1. Department of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, Amarillo, TX 79106, USA
2. Center for Blood Brain Barrier Research, Texas Tech University Health Sciences Center, Amarillo, TX 79106, USA
Interests: neuroscience; toxicology; in vitro modeling; biomarkers; molecular biology; redox metabolism
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Chemoprevention is one of the important strategies that can be employed in fighting many different types of cancer. Much research in recent years has been devoted to the understanding of biological pathways that can be utilized in chemopreventive strategies and the validation of possible chemopreventive targets using in vitro and in vivo models. Despite a large volume of research, some cancers, including lung cancer, are still lacking effective chemopreventive agents. In this Issue, we are welcoming reports of the most recent advances in the identification of novel targets for chemoprevention; the design of novel ligands with the ability to interfere with carcinogenesis and their evaluation in vitro and in vivo; as well as papers describing novel in vitro and in vivo models for developing chemopreventive agents.

Dr. Nadezhda German
Dr. Constatninos Mikelis
Assoc. Prof. Luca Cucullo
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

  • Chemoprevention
  • Rational drug design
  • Prostate cancer
  • Lung cancer
  • Breast cancer
  • Chemopreventive pathways
  • Tumorogenesis
  • carcinogenesis

Published Papers (1 paper)

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Review

17 pages, 8519 KiB  
Review
Structure Activity Relationship of Key Heterocyclic Anti-Angiogenic Leads of Promising Potential in the Fight against Cancer
by Hossam Nada, Ahmed Elkamhawy and Kyeong Lee
Molecules 2021, 26(3), 553; https://doi.org/10.3390/molecules26030553 - 21 Jan 2021
Cited by 13 | Viewed by 2715
Abstract
Pathological angiogenesis is a hallmark of cancer; accordingly, a number of anticancer FDA-approved drugs act by inhibiting angiogenesis via different mechanisms. However, the development process of the most potent anti-angiogenics has met various hurdles including redundancy, multiplicity, and development of compensatory mechanisms by [...] Read more.
Pathological angiogenesis is a hallmark of cancer; accordingly, a number of anticancer FDA-approved drugs act by inhibiting angiogenesis via different mechanisms. However, the development process of the most potent anti-angiogenics has met various hurdles including redundancy, multiplicity, and development of compensatory mechanisms by which blood vessels are remodeled. Moreover, identification of broad-spectrum anti-angiogenesis targets is proved to be required to enhance the efficacy of the anti-angiogenesis drugs. In this perspective, a proper understanding of the structure activity relationship (SAR) of the recent anti-angiogenics is required. Various anti-angiogenic classes have been developed over the years; among them, the heterocyclic organic compounds come to the fore as the most promising, with several drugs approved by the FDA. In this review, we discuss the structure–activity relationship of some promising potent heterocyclic anti-angiogenic leads. For each lead, a molecular modelling was also carried out in order to correlate its SAR and specificity to the active site. Furthermore, an in silico pharmacokinetics study for some representative leads was presented. Summarizing, new insights for further improvement for each lead have been reviewed. Full article
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