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Molecules
Special Issues
Design, Synthesis and Evaluation of New Antitumor Agents
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Design, Synthesis and Evaluation of New Antitumor Agents

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

Deadline for manuscript submissions: closed (30 April 2022) | Viewed by 4697

Special Issue Editor

Prof. Dr. David Barker

E-Mail Website
Guest Editor
School of Chemical Sciences, University of Auckland, Private Bag 92019, Auckland, New Zealand
Interests: medicinal chemistry; natural products total synthesis; asymmetric synthesis; bioactive natural products; polymeric materials; anticancer treatments; synthesis from biowaste-derived materials; isotopically labelled materials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In many countries around the world, cancer is the leading cause of death. This is particularly the case in developed countries which have an increasing average age of their populations. Despite great advances in its treatment, with numerous advances in chemotherapy, surgeries and radiation treatments, there are still many cancers which have poor patient prognosis and limited available therapies. There is therefore still a real need to develop new treatments for cancer, especially treatments with fewer side-effects than older classical treatments.

In this Special Issue, we wish to focus on all areas related to the development of new anti-tumour agents. This includes the discovery, design, synthesis and biological testing of novel treatments for cancer.

Prof. Dr. David Barker
Guest Editor

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

  • Drug design
  • Anti-cancer
  • Anti-neoplastic
  • Anti-tumour
  • Synthesis
  • Natural products
  • High throughput Screening
  • Structural activity relationship (SAR)
  • Biochemical assays
  • Cell-based assays
  • Drug delivery systems

Published Papers (2 papers)

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Research

17 pages, 2767 KiB  
Article
Biphenyl Ether Analogs Containing Pomalidomide as Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction
by Shabnam Shaabani, Louis Gadina, Ewa Surmiak, Zefeng Wang, Bidong Zhang, Roberto Butera, Tryfon Zarganes-Tzitzikas, Ismael Rodriguez, Justyna Kocik-Krol, Katarzyna Magiera-Mularz, Lukasz Skalniak, Alexander Dömling and Tad A. Holak
Molecules 2022, 27(11), 3454; https://doi.org/10.3390/molecules27113454 - 27 May 2022
Cited by 4 | Viewed by 2340
Abstract
New biphenyl-based chimeric compounds containing pomalidomide were developed and evaluated for their activity to inhibit and degrade the programmed cell death-1/programmed cell death- ligand 1 (PD-1/PD-L1) complex. Most of the compounds displayed excellent inhibitory activity against PD-1/PD-L1, as assessed by the homogenous time-resolved [...] Read more.
New biphenyl-based chimeric compounds containing pomalidomide were developed and evaluated for their activity to inhibit and degrade the programmed cell death-1/programmed cell death- ligand 1 (PD-1/PD-L1) complex. Most of the compounds displayed excellent inhibitory activity against PD-1/PD-L1, as assessed by the homogenous time-resolved fluorescence (HTRF) binding assay. Among them, compound 3 is one of the best with an IC50 value of 60 nM. Using an ex vivo PD-1/PD-L1 blockade cell line bioassay that expresses human PD-1 and PD-L1, we show that compounds 4 and 5 significantly restore the repressed immunity in this co-culture model. Western blot data, however, demonstrated that these anti-PD-L1/pomalidomide chimeras could not reduce the protein levels of PD-L1. Full article
(This article belongs to the Special Issue Design, Synthesis and Evaluation of New Antitumor Agents)
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9 pages, 881 KiB  
Article
Disruption of Crystal Packing in Thieno[2,3-b]pyridines Improves Anti-Proliferative Activity
by Natalie A. Haverkate, Euphemia Leung, Lisa I. Pilkington and David Barker
Molecules 2022, 27(3), 836; https://doi.org/10.3390/molecules27030836 - 27 Jan 2022
Cited by 1 | Viewed by 1859
Abstract
3-Amino-2-arylcarboxamido-thieno[2,3-b]pyridines have been shown to have anti-proliferative activity, but are also known to have poor solubility. This has been previously proposed to be due to their extensive planarity, which allows for intermolecular stacking and crystal packing. We herein report the synthesis [...] Read more.
3-Amino-2-arylcarboxamido-thieno[2,3-b]pyridines have been shown to have anti-proliferative activity, but are also known to have poor solubility. This has been previously proposed to be due to their extensive planarity, which allows for intermolecular stacking and crystal packing. We herein report the synthesis of fifteen novel thieno[2,3-b]pyridines that have incorporated bulky, but easily cleavable, ester and carbonate functional groups in an effort to decrease crystal packing. The addition of these ‘prodrug-like’ moieties into the thieno[2,3-b]pyridine resulted in compounds with increased activity against HCT-116 colon cancer cells and the triple-negative breast cancer cell line MDA-MB-231. Full article
(This article belongs to the Special Issue Design, Synthesis and Evaluation of New Antitumor Agents)
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