Neoplasm metastases involve a fixed cascade of pathological processes responsible for 90% cancer mortality worldwide. However, currently neoplasm metastases are poorly managed in humans for lack of good drug targets. To change this situation, new drug targets must be established. Aberrantly tumor sialylated study is one of potential drug targets, which has been involved for a half century. Many new discoveries show promising outcomes in experimental models. Since neoplasm tissues often contain higher levels of total sialic acids (sia), sialic acids-containing antigens, several types of sialic acid analogue, such as N-glycolylneuraminic acids, growing attentions of sia-related tumor diagnostics and therapeutics are needed to work with new cancer treatment approaches. Previously some compounds that inhibit pathologic pathways of sialic acids in tumor movements in vitro and tumor metastasis in animal tumor models were found. This type of pharmacological limitations of cancer metastasis treatments can be possibly solved by future glycome/metabolomics technology utilities. As the "central dogma" of glycobiology is still unknown to us, some fundamental questions related to carbohydrate itself are even more important comparing with individual experimental discoveries. In addition, mathematicor physics-majored talents in this topic might catalyze these new discoveries. In this review, we document these strings of lab biologic evidence, drug development updating and close relationships between cancer pathological profiles and therapeutic targets/benefits in clinics.