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Many macro and micro species, from terrestrial and aquatic environments, produce structurally unique compounds and, in many countries, still are the primary sources of medicines. In fact, secondary metabolites are an important source of chemotherapeutic agents but are also lead compounds for synthetic modification and the optimization of biological activity. Therefore, the exploitation of secondary metabolites, or their inspired synthetic compounds, offers excellent opportunities for the pharmaceutical industry. This Medicines Special Issue focuses on the great potential of secondary metabolites for therapeutic application. The Special Issue contains 16 articles reporting relevant experimental results, and an overview of bioactive secondary metabolites, their biological effects, and new methodologies that improve and accelerate the process of obtained lead compounds with regard to new drug development. We would like to thank all 83 authors, from all over the world, for their valuable contributions to this Special Issue.

antitumor --- triterpenoids --- seaweeds --- diterpenes --- Boswellia --- antioxidant activity --- antiplasmodial --- Maytenus chiapensis --- phenolic derivatives --- secondary metabolites --- medicinal applications --- Malus x domestica --- pectin --- cytotoxic activity --- xanthine oxidase --- phytochemistry --- antioxidant --- Scabiosa --- sugars --- sargaquinoic acid --- pentacyclic triterpenoids --- analysis --- antimicrobial and anticancer activity --- iridoids --- Tuscany --- GC-MS --- (-)-rabdosiin --- kratom --- plant defense --- cembranoids --- tingenone --- deoxypodophyllotoxin --- anticancer --- pristimerin --- inflammation --- boswellic acids --- plants --- anti-inflammatory --- legalization --- Mitragyna speciosa --- Ocimum sanctum --- cordycepin --- cytotoxic --- medicine --- Artemisia species --- antimicrobial activity --- lignans --- Artemisia vachanica --- Cordyceps militaris --- frankincense --- ancient varieties --- sargahydroquinoic acid --- Tajikistan --- antiSMASH --- ABTS --- polyphenols --- therapeutics --- infectious diseases --- antibacterial --- nutraceutics --- total phenolics --- LC-MS/MS --- innate immunity --- HPLC-PAD --- sarganaphthoquinoic acid --- biosynthetic gene clusters --- DPPH --- EGCG --- cneorubenoids --- PPAR-? --- bowel diseases --- amentoflavone --- molecular docking --- sargachromenoic acid --- cannabinoids --- flavonoids --- essential oils --- TCM --- HPLC-PDA --- ascorbic acid --- antioxidants --- Lamiaceae --- nanoemulsion --- malaria --- therapeutic uses --- quinonemethide triterpenoids --- artemisinin --- natural products --- biological activities --- FRAP --- toxicology --- defensins --- Celastraceae --- cannabis --- vector control --- Juniperus --- analytical determination