title: Heterocyclic Anticancer Compounds: Recent Advances and the Paradigm Shift towards the Use of Nanomedicine's Tool Box.
abstract: The majority of heterocycle compounds and typically common heterocycle fragments present in most pharmaceuticals currently marketed, alongside with their intrinsic versatility and unique physicochemical properties, have poised them as true cornerstones of medicinal chemistry. Apart from the already marketed drugs, there are many other being investigated for their promising activity against several malignancies. In particular, anticancer research has been capitalizing on the intrinsic versatility and dynamic core scaffold of these compounds. Nevertheless, as for any other promising anticancer drugs, heterocyclic compounds do not come without shortcomings. In this review, we provide for a concise overview of heterocyclic active compounds and families and their main applications in medicine. We shall focus on those suitable for cancer therapy while simultaneously addressing main biochemical modes of action, biological targets, structure-activity relationships as well as intrinsic limitation issues in the use of these compounds. Finally, considering the advent of nanotechnology for effective selective targeting of drugs, we shall discuss fundamental aspects and considerations on nanovectorization of such compounds that may improve pharmacokinetic/pharmacodynamic properties of heterocycles.
authors.affiliation: UCIBIO, Departamento de Ciências da Vida, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, Campus de Caparica, 2829-516 Caparica, Portugal. pf.martins@campus.fct.unl.pt.
authors.forename: Pedro
authors.initials: P
authors.lastname: Martins
authors.affiliation: UCIBIO, Departamento de Ciências da Vida, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, Campus de Caparica, 2829-516 Caparica, Portugal. joao.af.jesus@gmail.com.
authors.forename: João
authors.initials: J
authors.lastname: Jesus
authors.affiliation: UCIBIO, Departamento de Ciências da Vida, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, Campus de Caparica, 2829-516 Caparica, Portugal. sg.santos@campus.fct.unl.pt.
authors.forename: Sofia
authors.initials: S
authors.lastname: Santos
authors.affiliation: UCIBIO, Departamento de Ciências da Vida, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, Campus de Caparica, 2829-516 Caparica, Portugal. luismrraposo@gmail.com.
authors.forename: Luis R
authors.initials: LR
authors.lastname: Raposo
authors.affiliation: UCIBIO, Departamento de Ciências da Vida, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, Campus de Caparica, 2829-516 Caparica, Portugal. catromar@fct.unl.pt.
authors.forename: Catarina
authors.initials: C
authors.lastname: Roma-Rodrigues
authors.affiliation: UCIBIO, Departamento de Ciências da Vida, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, Campus de Caparica, 2829-516 Caparica, Portugal. pmvb@fct.unl.pt.
authors.forename: Pedro Viana
authors.initials: PV
authors.lastname: Baptista
authors.affiliation: UCIBIO, Departamento de Ciências da Vida, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, Campus de Caparica, 2829-516 Caparica, Portugal. ma.fernandes@fct.unl.pt.|Centro de Química Estrutural, Complexo 1, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, Portugal. ma.fernandes@fct.unl.pt.
authors.forename: Alexandra R
authors.initials: AR
authors.lastname: Fernandes
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000494:pharmacology*; D006801:Humans; D050997:Nanomedicine; D009369:Neoplasms / Q000188:drug therapy*
chemical_list: D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds
keywords: cancer therapy; drug delivery; heterocyclic compounds; nanomedicine; oxygen and nitrogen-based heterocycles