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Biomolecules
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Heterocyclic Compounds as Novel Anti-Cancer Agents and Their Mechanisms of...
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Heterocyclic Compounds as Novel Anti-Cancer Agents and Their Mechanisms of Action

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Molecular Medicine".

Deadline for manuscript submissions: 31 August 2025 | Viewed by 1032

Special Issue Editors

Dr. Chandra Mishra

E-Mail Website
Guest Editor
Department of Pharmacology & Chemical Biology, Baylor College of Medicine, Baylor Plaza, Houston, TX 77030, USA
Interests: small-molecule drug discovery; medicinal chemistry; proteolysis-targeting chimeras (PROTACs); targeted protein degradation (TPD); chemical biology; CNS drug discovery
Special Issues, Collections and Topics in MDPI journals
Dr. Dnyaneshwar N. Garad

E-Mail Website
Guest Editor
Department of Pharmacology & Chemical Biology, Baylor College of Medicine, Baylor Plaza, Houston, TX 77030, USA
Interests: organic chemistry; medicinal chemistry; small-molecule drug discovery; chemical biology

Special Issue Information

Dear Colleagues,

The development of next-generation cancer therapies is crucial for identifying new targets and advancing precision oncology. Cancer remains a major concern and a leading cause of human suffering. Every year, the number of cancer cases and deaths continues to rise, posing a significant danger to public health and healthcare systems worldwide. The study of pathways, mechanisms, and structures of anticancer chemical compounds has played a crucial role in cancer prevention and treatment. Identifying different tumor cell lines and assessing the impact of natural and synthetic anticancer compounds has led to significant success. However, current therapy still faces challenges, such as the toxicity of anticancer agents and the damage they cause to normal tissues. There is an urgent need to develop potential anticancer agents with fewer off-target effects. This call for submissions includes novel anticancer heterocyclic compounds from both synthetic and natural sources, validated through in vitro or in vivo assessments of their mechanisms of action. Authors are invited to submit original research articles and review articles focused on heterocyclic compounds as novel anti-cancer agents and their mechanisms of action.

Dr. Chandra Mishra
Dr. Dnyaneshwar N. Garad
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. Biomolecules is an international peer-reviewed open access monthly 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

  • heterocyclic compounds
  • anticancer
  • synthetic
  • natural

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Published Papers (2 papers)

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Research

15 pages, 2350 KiB  
Article
ONC201 (Dordaviprone) Induces Integrated Stress Response and Death in Cervical Cancer Cells
by Sneha O. Pathak and Sonal M. Manohar
Biomolecules 2025, 15(4), 463; https://doi.org/10.3390/biom15040463 - 21 Mar 2025
Viewed by 173
Abstract
Cervical cancer is a leading cause of death in women globally. Systemic chemotherapy offers only limited therapeutic benefit for advanced-stage disease due to toxicity and drug resistance. ONC201 (also known as TIC10 or dordaviprone) is a TRAIL (TNF-Related Apoptosis-Inducing Ligand) and cIpP (caseinolytic [...] Read more.
Cervical cancer is a leading cause of death in women globally. Systemic chemotherapy offers only limited therapeutic benefit for advanced-stage disease due to toxicity and drug resistance. ONC201 (also known as TIC10 or dordaviprone) is a TRAIL (TNF-Related Apoptosis-Inducing Ligand) and cIpP (caseinolytic protease) agonist currently in Phase II clinical trials for different types of cancer. In the present study, we investigated the anticancer potential of ONC201 in HPV-positive cervical cancer cell lines. ONC201 exerted significant cytotoxicity and inhibited the clonogenic potential of cervical cancer cells. It induced integrated stress response along with S/G2-M arrest and apoptosis in both cell lines. Yet, surprisingly, well-known targets of ONC201 viz. TRAIL, DR5 (death receptor 5) and cIpP were found to be upregulated only in HeLa but not in SiHa cells in response to ONC201 treatment. In addition, expression of BNIP3 and Beclin-1 (both involved in regulation of autophagy) increased in response to certain doses of ONC201. Furthermore, ONC201 exhibited synergism in combination with standard drugs against cervical cancer cells. This study provides a proof of concept for the anticancer activity of versatile drug ONC201 against cervical cancer cells and also delineates its mechanism of action. Full article
(This article belongs to the Special Issue Heterocyclic Compounds as Novel Anti-Cancer Agents and Their Mechanisms of Action)
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36 pages, 13267 KiB  
Article
Synthesis, Antiproliferative Activity, and ADME Profiling of Novel Racemic and Optically Pure Aryl-Substituted Purines and Purine Bioisosteres
by Martina Piškor, Astrid Milić, Sanja Koštrun, Maja Majerić Elenkov, Petra Grbčić, Sandra Kraljević Pavelić, Krešimir Pavelić and Silvana Raić-Malić
Biomolecules 2025, 15(3), 351; https://doi.org/10.3390/biom15030351 - 28 Feb 2025
Viewed by 321
Abstract
The aim of this study was to synthesize new racemic and optically pure aryl-substituted purine bioisosteres using ultrasound-assisted Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition. Regioselective synthesis of α-azido alcohols was applied to afford heterocycles with a 2-hydroxyeth-1-yl linker. Catalytic asymmetric synthesis using halohydrin dehalogenase in [...] Read more.
The aim of this study was to synthesize new racemic and optically pure aryl-substituted purine bioisosteres using ultrasound-assisted Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition. Regioselective synthesis of α-azido alcohols was applied to afford heterocycles with a 2-hydroxyeth-1-yl linker. Catalytic asymmetric synthesis using halohydrin dehalogenase in the ring-opening of epoxides gave enantioenriched azido alcohols, which subsequently afforded R- and S-enantiomers of purine and pyrrolo[2,3-d]pyrimidines with a 1-hydroxyeth-2-yl linker. The newly synthesized compounds were evaluated in vitro for their antiproliferative activity against four malignant tumor cell lines. The influence of regioisomerism and the stereochemistry of the hydroxyethyl group, as well as a N-heterocyclic scaffold linked to the aryl moiety on cytostatic activity was evaluated. Of all the compounds tested, purine 40a and pyrrolo[2,3-d]pyrimidine 45a derivatives with p-trifluoromethyl-substituted aryl connected to 1,2,3-triazole via a 2-hydroxyeth-1-yl spacer showed promising submicromolar antiproliferative activity. In addition, compound 45a exhibited selectivity towards the tumor cell line, with a selectivity index (SI) of 40, moderate clearance, and good membrane permeability. Full article
(This article belongs to the Special Issue Heterocyclic Compounds as Novel Anti-Cancer Agents and Their Mechanisms of Action)
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