Comments section impact of adding pyridine based antitumoral compounds towards colchicine

comments section impact of adding pyridine based antitumoral compounds towards colchicine -

The tubulin inhibitors are among the most effective agents anti- cancer, anti-parasitic and herbicides. Their vascular disruptive activity has recently attracted the focus of research because it causes anti-cancer effects at much lower doses than other toxic agents. The colchicine site of tubulin is located in a hydrophobic region at the interface of the α-tubulin, β-dimer. binding ligands of the colchicine site occupy different pockets and to different types of interactions with the protein. colchicine site agents are structurally simple, and synthetically available anti-tubulin agents are in active development. But these agents suffer from poor pharmacokinetics. The incorporation of pyridine and related nitrogen heterocycles in the structures of colchicine site of agents led to new scaffolds assets, improved potencies and pharmacokinetic improvements for binding with ligands of the colchicine site.
This article critically examines the impact of these changes in the field and in the future prospects of this class of agents clinical success. The colchicine binding drugs were classified according to their modes described or alleged link and impact of pyridine and fragments related to the business for each class of compounds is discussed on the basis of the structure - property and structure - activity relationships, and the X-ray structures when available. Special emphasis was made on drugs advancing in clinical trials and evidence of design changes. From this analysis, a new insight into the targeting tubulin is highlighted as well as the future prospects for the development of specific agents in a similar website.