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Pharmaceuticals
Special Issues
Novel Anti-Proliferative Agents 2024
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Special Issue "Novel Anti-Proliferative Agents 2024"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 25 June 2024 | Viewed by 577

Special Issue Editor

Prof. Dr. Valentina Onnis

E-Mail Website1 Website2
Guest Editor
Department of Life and Environmental Sciences, Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, University Campus, I-09042 Monserrato, Italy
Interests: medicinal chemistry; nitrogen heterocycles; antiproliferative compounds; enzyme inhibitors
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer is one of the most widely spread and complex forms of disease, as cancer cells are distinguished from healthy cells due to their altered proliferation and survival. In the past three decades, the National Cancer Institute (NCI) alone has screened millions of small molecules for potential anticancer activity. Despite a number of conventional cytotoxic approaches having been developed, their limited effectiveness, in accordance with the heterogeneity of cancer cells, prompts the constant search for novel natural or synthetic compounds with properties involved in growth inhibition or tumor cell activity reduction.

This Special Issue of Pharmaceuticals invites both reviews and original articles regarding basic, preclinical and clinical studies on antiproliferative chemical entities.

I look forward to receiving your contributions.

Prof. Dr. Valentina Onnis
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. Pharmaceuticals 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 2900 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

  • medicinal chemistry
  • drug discovery
  • natural compounds
  • synthetic compounds
  • organic synthesis
  • bioactivity
  • anticancer drugs
  • antiproliferative activity

Published Papers (1 paper)

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Research

13 pages, 4197 KiB  
Communication
Design, Synthesis, In Vitro, and In Silico Studies of New N5-Substituted-pyrazolo[3,4-d]pyrimidinone Derivatives as Anticancer CDK2 Inhibitors
by
Waheed A. Zaki
,
Selwan M. El-Sayed
,
Mohamed Alswah
,
Ahmed El-Morsy
,
Ashraf H. Bayoumi
,
Abrahman S. Mayhoub
,
Walaa H. Moustafa
,
Aeshah A. Awaji
,
Eun Joo Roh
,
Ahmed H.E. Hassan
and
Kazem Mahmoud
Pharmaceuticals 2023, 16(11), 1593; https://doi.org/10.3390/ph16111593 - 11 Nov 2023
Viewed by 491
Abstract
CDK2 is a key player in cell cycle processes. It has a crucial role in the progression of various cancers. Hepatocellular carcinoma (HCC) and colorectal cancer (CRC) are two common cancers that affect humans worldwide. The available therapeutic options suffer from many drawbacks [...] Read more.
CDK2 is a key player in cell cycle processes. It has a crucial role in the progression of various cancers. Hepatocellular carcinoma (HCC) and colorectal cancer (CRC) are two common cancers that affect humans worldwide. The available therapeutic options suffer from many drawbacks including high toxicity and decreased specificity. Therefore, there is a need for more effective and safer therapeutic agents. A series of new pyrazolo[3,4-d]pyrimidine analogs was designed, synthesized, and evaluated as anticancer agents against the CRC and HCC cells, HCT116, and HepG2, respectively. Pyrazolo[3,4-d]pyrimidinone derivatives bearing N5-2-(4-halophenyl) acetamide substituents were identified as the most potent amongst evaluated compounds. Further evaluation of CDK2 kinase inhibition of two potential cytotoxic compounds 4a and 4b confirmed their CDK2 inhibitory activity. Compound 4a was more potent than the reference roscovitine regarding the CDK2 inhibitory activity (IC50 values: 0.21 and 0.25 µM, respectively). In silico molecular docking provided insights into the molecular interactions of compounds 4a and 4b with important amino acids within the ATP-binding site of CDK2 (Ile10, Leu83, and Leu134). Overall, compounds 4a and 4b were identified as interesting CDK2 inhibitors eliciting antiproliferative activity against the CRC and HCC cells, HCT116 and HepG2, respectively, for future further investigations and development. Full article
(This article belongs to the Special Issue Novel Anti-Proliferative Agents 2024)
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