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Special Issue "Cancer and Tuberculosis Drug Discovery: A Theme Issue in Honor of Prof. William A. Denny"

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

Deadline for manuscript submissions: 31 December 2020.

Special Issue Editors

Prof. Larry Wakelin
Guest Editor
University of New South Wales (UNSW) Australia, Sydney, Australia
Interests: medicinal chemistry; cancer drug discovery; DNA-targeted cytotoxins; DNA–ligand interactions
Prof. Dr. Sandra Gemma
Guest Editor
Department of Biotechnology, chemistry and pharmacy, University of Siena via Aldo Moro 2, 53100 Siena, Italy
Interests: medicinal chemistry; small molecules, drug discovery; structure-activity relationships; anti-infective agents; parasitic diseases; chemotherapeutics; synthesis of biologically active compounds
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Special Issue Information

Dear Colleagues,

Professor William (Bill) Denny was born in Malvern, UK, and has a PhD in organic chemistry from the University of Auckland, New Zealand. In addition to brief periods at Oxford University and at UC San Diego, he has worked at the University of Auckland in the Auckland Cancer Society Research Centre (ACSRC), where he has been Director from 1981 to today. He has mentored 80-plus PhD candidates and post-doctoral scientists in his laboratory and, to date, has published with them 720 scientific papers and more than 130 patent applications.

With the primary goal of developing novel drugs for cancer therapy and infectious diseases, Professor Denny has endeavoured, with colleagues, to develop a group in the ACSRC that covers the necessary skills (computer modelling, medicinal chemistry, pharmacology, cancer and radiation biology, immunology and clinical oncology) for drug design and development. He sought in particular to build commercial collaborations, with both existing pharma companies, and via new start-up companies, out of the ACSRC’s research. He has been a scientific co-founder of Proacta Inc (San Diego), Pathway Therapeutics Ltd (San Francisco) and KEA Therapeutics (Auckland). So far, this has resulted in 18 drugs from the ACSRC being taken to clinical trial.

Professor Denny’s own areas of research have included topoisomerase poisons, DNA-targeted alkylating agents, DNA methyltransferase inhibitors, kinase inhibitors (EGFR, PI3K, CSF1R), and hypoxia-activated prodrugs for cancer therapy and inhibitors of deazaflavin-dependent nitroreductase and ATP synthase for tuberculosis. Professor Denny’s awards include the UK Royal Society of Chemistry’s Lectureship (1999) and Adrien Albert Medal (2005), the University of Auckland Vice-Chancellor’s Commercialisation Medal (2012) and the American Chemical Society Biennial Medicinal Chemistry Award (2014). He is currently an associate editor of the Journal of Medicinal Chemistry (American Chemical Society) and of Anti-Cancer Agents in Medicinal Chemistry (Bentham).

Professor Denny, through his outstanding leadership in the medicinal chemistry of a wide range of classes of cancer drugs, as well as drugs for tuberculosis, and by his skills in chaperoning lead compounds to clinical candidates, has developed the ACSRC into a world-renowned academic centre for drug discovery and development. By his extraordinary efforts, and those of his senior colleagues, he has provided a paradigm for how academic research groups can make a material contribution to the treatment of the most serious human diseases. He is an inspiration to all, and on the occasion of his retirement as ACSRC director, we are pleased to invite you to submit a publication for this Special Issue.

Prof. Larry Wakelin
Prof. Dr. Sandra Gemma
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at 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 papers will be 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 2000 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.


  • DNA-targeted cytotoxins
  • Kinase inhibitors as cancer drugs
  • Hypoxia-activated pro-drugs for cancer therapy
  • Nitroreductase and ATP synthase inhibitors for tuberculosis

Published Papers (1 paper)

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Open AccessArticle
Synergistic Activity of Nitroimidazole-Oxazolidinone Conjugates against Anaerobic Bacteria
Molecules 2020, 25(10), 2431; (registering DOI) - 22 May 2020
The introductions of the bicyclic 4-nitroimidazole and the oxazolidinone classes of antimicrobial agents represented the most significant advancements in the infectious disease area during the past two decades. Pretomanid, a bicyclic 4-nitroimidazole, and linezolid, an oxazolidinone, are also part of a combination regimen [...] Read more.
The introductions of the bicyclic 4-nitroimidazole and the oxazolidinone classes of antimicrobial agents represented the most significant advancements in the infectious disease area during the past two decades. Pretomanid, a bicyclic 4-nitroimidazole, and linezolid, an oxazolidinone, are also part of a combination regimen approved recently by the US Food and Drug Administration for the treatment of pulmonary, extensively drug resistant (XDR), treatment-intolerant or nonresponsive multidrug-resistant (MDR) Mycobacterium tuberculosis (TB). To identify new antimicrobial agents with reduced propensity for the development of resistance, a series of dual-acting nitroimidazole-oxazolidinone conjugates were designed, synthesized and evaluated for their antimicrobial activity. Compounds in this conjugate series have shown synergistic activity against a panel of anaerobic bacteria, including those responsible for serious bacterial infections. Full article
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Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

1. Stephen Neidle, University College London, UK
2. Hollis Showalter, University of Michigan, Ann Arbor, USA
3. Zhenkun Ma, Global Alliance for TB Drug Development, New York, USA
4. Jeff Bruce Smaill, University of Auckland, New Zealand
5. Adam Patterson, University of Auckland, New Zealand
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