Introduction: Natural products have been used in clinical therapeutics since time immemorial. It has been estimated that 56% of the lead compounds for medicines in the British National Formulary are natural products or are derived from natural products. Materials: Despite the achievements of synthetic chemistry and the advances towards rational drugs design, 50 important natural products are described which continue to be essential in providing medicinal compounds and as starting points for the development of synthetic analogues. Result: This article describes the phytoconstituents which are being used as lead compounds for the design, synthesis and development of Novel Drug Compounds. Conclusion: Despite the achievements of synthetic chemistry and the advances towards rational drugs design, natural products will continue to be important in three areas of drug discovery: they can be used as a target for production by biotechnology, as a source of new lead compounds of the novel chemical structure and as active ingredients for useful treatments following the traditional system of medicines. Moreover, along with biologically active primary plant metabolites, secondary compounds also serve additionally as chemical models or templates for the design and total synthesis of new drug entities.