Gnidia is a member genus of the Thymelaeaceae comprising of about 152 species; several members of which are frequently utilized for a wide variety of ailments like asthma, backache, nightmares, dropsy, boils, sores, induce blistering, treat bruises and burns, constipation, coughs, earache, epilepsy, headache, influenza and fevers, insanity, malaria, measles, pulmonary tuberculosis, poor appetite, smallpox, snake bites, sprains and fractures, tonsillitis, to stabilize heart conditions, stomach and chest complaints, toothache, ulcers and yellow fever and as broad-spectrum purgatives. Several Gnidia extracts have also shown antileukemic properties. Gnidia elaborates a vast array of biologically active compounds that are chemically diverse and structurally complex. More than 90 compounds have been isolated from different species of Gnidia. This review aims at giving an outline of the variety of the secondary metabolites produced by Gnidia, as well as their biological activities. The genus Gnidia is rich in diterpene esters, coumarins, flavonoids, chromones, lignans, and neolignans. Phytochemical studies on some Gnidia species indicated the presence of toxic diterpene esters of daphnane type, which are the main types of plant orthoesters and have remarkable biological activities, such as antineoplastic and cytotoxic. These gnidia compounds may be helpful as leads in the synthesis of analogs for treating various ailments.