The marine microenvironment harbors a number of unique species of organisms that produce a plethora of compounds that help mankind to cure a wide range of diseases. The diversity of products from the ocean bed serve as potentially healing materials and inert vehicles carrying the drug of interest to the target site. Several composites still lay undiscovered under the blue canopy, which can provide treatment for untreated diseases that keep haunting the earth periodically. Cancer is one such disease that has been of interest to several eminent scientists worldwide over the decades due to the heterogenic complexity involved in the disease pathophysiology. Due to extensive globalization and environmental changes, cancer has become a lifestyle disease that is continuously increasing exponentially in the current decade. This ailment requires a definite remedy that treats by causing minimal damage to the normal cells of the body. The application of nanotechnology in medicine has opened up new avenues of research in targeted therapeutics due to their highly malleable characteristics. Marine waters contain an immense ionic environment that succours the production of distinct nanomaterials with exceptional character, which yield molecules highly flexible to modifications, thus facilitating the engineering of targeted biomolecules. This review provides a short insight into an array of marine biomolecules that can be probed into cancer nano-therapeutics sparing healthy cells.