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Abstract
Natural products have played a significant role in the drug discovery especially in the area of cancer. Over the period of 1940-2010, 50% of the small molecules introduced as anticancer agents were either natural products or directly derived therefrom. In one of the ongoing collaborative project to identify anticancer leads, the Mycosynthetix library, representing over 55,000 accessions of filamentous fungi, is being examined systematically. The bioactive-guided fractionation methodology is adopted for the isolation and purification of cytotoxic lead compounds. The first chapter describes the isolation of cytotoxic secondary metabolites using bio-activity guided fractionation scheme. As part of ongoing investigations of filamentous fungi for anticancer drug leads, a bioactivity-guided fractionation methodology utilizes chloroform in the initial extraction and fractionation processes. Due to the concerns regarding human health and halogenated waste associated with chloroform, an attempt was made to replace it with more environmentally benign ester-based solvents. In this project, ethyl acetate, methyl acetate and ethyl formate were used in the initial stages of extractions and processing. The extraction efficiency of these was compared versus chloroform using two well-studied fungi.