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Calanolides are naturally occurring pyranocoumarins found particularly in Calophyllum species (family Clusiaceae/ Guttiferae), and are well known for their potent anti-human immunodeficiency virus (HIV) activity. Various preclinical and clinical studies with this class of compounds are going on, and the National Cancer Institute (NCI) has been playing an active and supportive role in this regard. The present review covers an up-to-date literature of naturally occurring calanolides in view of their anti-HIV potential and total syntheses including information on related patents.