Abstract
The novel or designer metabolites produced by fungal endophytes are increasingly recognized by natural chemists due to their diverse structures and as candidates for drug discovery and development. Many of the metabolites belong to different classes i.e. alkaloids, benzopyranones, coumarins, chromones, cytochalasines, enniatines, isocoumarin derivatives, quinones, peptides, phenols, phenolic acids, semiquinones, steroids, terpenoids, xanthones and lactones. One of the most widely studied endophytic genera is Pestalotiopsis, from which more than 140 metabolites are reported with antimicrobial, antioxidant and antitumor activities. Besides reviewing the advances made in identifying bioactive metabolites with drug development potential from endophytic fungi, this chapter discusses possibilities and bottlenecks involved in employment of endophytic fungi and their products by the pharmaceutical industry. Furthermore, issues involved in anti-infective discovery and timeline of drug development are discussed in the view of developing new drug compounds from endophytic products.