Design, Synthesis, Evaluation and Biopharmaceutical Uses of Imatinib, Nilotinib and Their Analogues
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: closed (25 March 2025) | Viewed by 1156
Special Issue Editors
Interests: supramolecular chemistry; organic sythesis; protein kinase inhibitors; molecular docking; dendrimers
Interests: athophysiology of atherosclerosis; platelets; thrombosis; antiatherogenic and antithrombotic effects; protein kinase inhibitors; cancer-associated thrombosis
Special Issue Information
Dear Colleagues,
Cancer is the leading cause of death worldwide, accounting for nearly 10 million deaths per year, as stated by the World Health Organization. Nearly one in six deaths is caused by cancer, with the most common being breast, lung, colon and rectum and prostate cancers.
In 2001, a revolutionary drug, which turned out to be very effective for the treatment of chronic myeloid leukemia (CML), was approved and released, changing the approach of cancer’s target therapy. The active substance, named Imatinib, was designed to deactivate a specific protein kinase, a fused BCR-ABL tyrosine protein kinase, terminating the cell signaling pathway that was responsible for the uncontrolled proliferation of white blood cells.
With Imatinib as the starting point, new molecules were synthesized with slight structural modifications, and they were evaluated for improved targeted anti-cancer properties. The innovative approach of blocking problematic protein kinase with low-molecular-weight molecules, usually by binding with the ATP-binding sites, led to the synthesis of a series of protein kinase inhibitors, and today, more than 65 of them have been approved or are under investigation in clinical trials as anti-cancer treatments. Among them is Nilotinib, a substance which has shown greater efficacy than Imatinib in patients with newly diagnosed Philadelphia chromosome-positive CML.
Pharmaceuticals launches a Special Issue, which focuses on state-of-the-art research works related to the following:
- The design of new synthetic approaches of Imatinib and Nilotinib;
- The development of their novel analogues;
- The evaluation of their biological properties and selectivity;
- Their biopharmaceutical uses.
We invite you to submit your original research articles for publication in this Special Issue.
Dr. Dimitrios Alivertis
Prof. Dr. Alexandros D. Tselepis
Dr. Pinelopi Voulgari
Guest Editors
Manuscript Submission Information
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Keywords
- cancer
- inhibitors
- Imatinib
- Nilotinib
- protein kinases
- target therapy
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