Pyrimidine and Purine Derivatives in Medicinal Chemistry

Dear Colleagues,

Pyrimidine and purine have been widely studied as privileged scaffolds in medicinal chemistry due to their broad applications in drug discovery programmes. This strategy has led some pyrimidine and purine derivatives to be approved by the FDA in the last decade as drugs for different treatments. Therefore, there have been constant efforts to obtain new derivatives containing these heterocyclic or bioisosteric moieties, with therapeutic properties with potential for the treatment of cancer, neurological and metabolic disorders, autoimmune, cardiovascular and infectious diseases. These properties are possible due to heterocycles’ presence in the biomolecules of all living organisms and important role in signalling pathways and metabolic and energetic processes. Thus, compounds that mimic these substrates will have certain pharmacological effects. From a molecular point of view, several therapeutic targets are modulated by these heterocycles, which could act as inhibitors of key enzymes such as tyrosine kinases (Bcr-Abl, BTK, ALK, etc.), serine/threonine kinases (CDKs), reverse transcriptase or receptor ligands for adenosine, histamine, FLT3 and JAK1-2, among others. However, despite the successful results achieved for the use of these small molecules as part of the therapeutic arsenal, many current treatments have continually lost efficacy due to certain mechanisms of resistance to this class of drugs promoted by mutations in the target proteins. For this reason, a search for new molecules to overcome these limitations is necessary.

Pharmaceuticals invites both original articles and reviews that address these challenges using pyrimidine and purine analogues and bioisosteres as part of new bioactive compounds in drug discovery, to be published as a Special Issue. Topics to be considered include drug design and synthesis and in vitro and in vivo studies, among others.

Dr. Cristian O. Salas
Dr. Christian Espinosa-Bustos
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. 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.

• pyrimidine derivatives
• purine derivatives
• synthetic methodology
• drug design
• bioisosteres
• cancer
• kinase inhibitors
• adenosine receptors
• structure–activity relationship
• molecular docking