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Exclusive Feature Papers in Synthetic Medicinal Chemistry
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Exclusive Feature Papers in Synthetic Medicinal Chemistry

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

Deadline for manuscript submissions: 31 December 2025 | Viewed by 1541

Special Issue Editors

Dr. Michail Christodoulou

E-Mail Website
Guest Editor
DeFENS, Department of Food, Environmental and Nutritional Sciences, Università degli Studi di Milano, Via Celoria 2, 20133 Milano, Italy
Interests: transition metal catalyzed reactions; synthetic methodologies to obtain bioactive molecules
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Constantinos Athanassopoulos

E-Mail Website
Guest Editor
Department of Chemistry, University of Patras, GR-26504 Patras, Greece
Interests: small organic molecules; natural products; anticancer and antibacterial agents; multitarget inhibitors; hybrids; bioconjugates
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue will provide up-to-date information on modern drug discovery, including antitumor and antibacterial compounds. The discovery of novel small-molecules with antitumor and antibacterial activity is a challenging field, and new compounds are synthesized yearly to overcome the drawbacks of the already synthesized analogs.

The developing resistance of tumor cells to a broad range of structurally and functionally different drugs and the demand for novel antimicrobials to treat life-threatening infections caused by multidrug-resistant bacteria are challenging obstacles to surpass.

New natural and natural-inspired compounds or synthetic compounds are the primary tools in the quiver of medicinal chemistry.

Contributions to this Special Issue may cover all advances related to drug discovery in the field of antitumor and antibacterial drugs, including new target identification, drug design, and lead optimization.

Dr. Michail Christodoulou
Prof. Dr. Constantinos Athanassopoulos
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

  • antitumor activity
  • antibacterial activity
  • natural and synthetic compounds

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (3 papers)

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Research

21 pages, 1771 KiB  
Article
Total Synthesis and Biological Evaluation of 22-Hydroxyacuminatine and the Related Natural Products Norketoyobyrine and Naucleficine
by Shohta Mizuno, Takashi Nishiyama, Hana Bessho, Tetsuya Nakamura, Tomoki Oe, Nanako Hayashi, Yuhzo Hieda, Toshio Motoyashiki, Toshiyuki Hata, Noriyuki Hatae and Tominari Choshi
Molecules 2025, 30(12), 2650; https://doi.org/10.3390/molecules30122650 - 19 Jun 2025
Viewed by 225
Abstract
Aromathecin compounds—which contain the same indolizine core structure as camptothecin-like compounds—are expected to show anticancer activity. Among them, 22-hydroxyacuminatine—which has a substituent on the E-ring of the pentacyclic scaffold—exhibits topoisomerase 1 inhibitory activity; therefore, the development of efficient methods for its synthesis has [...] Read more.
Aromathecin compounds—which contain the same indolizine core structure as camptothecin-like compounds—are expected to show anticancer activity. Among them, 22-hydroxyacuminatine—which has a substituent on the E-ring of the pentacyclic scaffold—exhibits topoisomerase 1 inhibitory activity; therefore, the development of efficient methods for its synthesis has been actively pursued. Herein, we report a versatile synthetic methodology for introducing various substituents on the E-ring, leading to the total synthesis of 22-hydroxyacuminatine as a model compound of the aromathecin family. The synthesis comprises the following key steps: the synthesis of an isoquinoline N-oxide via the thermal cyclization of 2-alkynylbenzaldehyde oxime, the subsequent Reissert–Henze-type reaction to yield an isoquinolone, and the construction of the indolizine moiety (CD-ring) through C–N bond formation via the Mitsunobu reaction. Consequently, a pentacyclic benz[6,7]indolizino[1,2-b]quinolin-11(13H)-one framework is obtained. Using this methodology, the total synthesis of the natural products norketoyobyrine and naucleficine and an intermediate of the latter, which are indoloquinolizidine-type alkaloids, was achieved, and their antiproliferative activity against HCT-116 human colon cancer cells and HepG2 human liver cancer cells was assessed. Naucleficine and its intermediate exhibited moderate antiproliferative activity against HCT-116 cells, with IC50 values of 55.58 and 41.40 μM, respectively. Full article
(This article belongs to the Special Issue Exclusive Feature Papers in Synthetic Medicinal Chemistry)
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25 pages, 2420 KiB  
Article
Synthesis, Stability, and Biological Evaluation of Novel Aminoderivatives Incorporating the Aza-Acridine Scaffold
by Maria Karelou, Anthi Panara, Eleftheria Chatziorfanou, Aikaterini F. Giannopoulou, Dimitrios J. Stravopodis, Evagelos Gikas and Ioannis K. Kostakis
Molecules 2025, 30(12), 2612; https://doi.org/10.3390/molecules30122612 - 16 Jun 2025
Viewed by 299
Abstract
Several new amino-substituted aza-acridine derivatives bearing one or two basic side chains have been designed and synthesized. Their anticancer activities were evaluated in vitro against two human cancer cell lines: T24 (urothelial bladder carcinoma, malignancy grade III) and WM266-4 (metastatic melanoma). Some of [...] Read more.
Several new amino-substituted aza-acridine derivatives bearing one or two basic side chains have been designed and synthesized. Their anticancer activities were evaluated in vitro against two human cancer cell lines: T24 (urothelial bladder carcinoma, malignancy grade III) and WM266-4 (metastatic melanoma). Some of the synthesized compounds induced significant antiproliferative effects, with WM266-4 cells appearing more susceptible than T24 cells. This apparent cell-type selectivity may reflect differences in the mutational profiles and molecular target landscapes between the two cancer models. A stability study under hydrolytic conditions, based on a validated method, indicated that the most active compounds were stable under aqueous conditions. Computational analysis further supported the stability of these analogs, providing insights into the structure–stability relationships of the synthesized compounds. Full article
(This article belongs to the Special Issue Exclusive Feature Papers in Synthetic Medicinal Chemistry)
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17 pages, 2057 KiB  
Article
Synthesis of Adenine Nucleosides with a Reactive (β-Iodovinyl)sulfone or (β-Keto)sulfone Group at the C2 Position and Their Polymerase-Catalyzed Incorporation into DNA
by A. Hasan Howlader, Richard Fernandez, Pawlos S. Tsegay, Yuan Liu and Stanislaw F. Wnuk
Molecules 2025, 30(6), 1358; https://doi.org/10.3390/molecules30061358 - 18 Mar 2025
Cited by 1 | Viewed by 541
Abstract
Iodosulfonylation of an ethynyl group at the C2 position of 2′-deoxyadenosine or adenosine with TsI provides (E)-2-(β-iodovinyl)sulfones. The latter undergo nucleophilic substitution with amines via an addition–elimination to give β-sulfonylvinylamines (enamines). Acid-catalyzed hydrolysis of the β-sulfonylvinylamines provides [...] Read more.
Iodosulfonylation of an ethynyl group at the C2 position of 2′-deoxyadenosine or adenosine with TsI provides (E)-2-(β-iodovinyl)sulfones. The latter undergo nucleophilic substitution with amines via an addition–elimination to give β-sulfonylvinylamines (enamines). Acid-catalyzed hydrolysis of the β-sulfonylvinylamines provides 2-(β-keto)sulfones, mechanistically different probes that react with alkyl halides, resulting in α-alkylation. Adenine nucleosides with a β-ketosulfone group at C2, during conversion to their 5′-triphosphate form, undergo an unexpected conversion to 2-carboxylic acid nucleotides. The 5′-triphosphate of 2′-deoxyadenosine-2-carboxylic acid was incorporated by a human DNA polymerase into a one-nucleotide gap DNA substrate. Full article
(This article belongs to the Special Issue Exclusive Feature Papers in Synthetic Medicinal Chemistry)
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