Chapter 10 - Dihydropyrimidinones inhibit proliferation and tumor growth

Abstract

Cancer accounts for the second principal reason for mortality at the global level after cardiovascular diseases with lung cancer continuing to remain the foremost cause of all cancer-linked deaths. Under these circumstances, the sighting of new therapeutic agents bears vital significance for the development of our medical management arsenal. DHMPs, heterocycles possessing a pyrimidine moiety in the annular nucleus, have received considerable attention in recent decades owing to their fascinating medicinal properties. Prepared via Biginelli reactions, DHMPs have attracted the attention of researchers for years together for their efficacy against cancer. In the present chapter, we document the inhibitory role of DHMPs and their derivatives in the proliferation of cells and tumor growth during carcinogenesis. This chapter covers the recent advancement of DHMP/thione moieties in drug development with special emphasis on cancer proliferation and tumor growth. Efforts have been made to identify the specific biological targets for exhibiting their antiproliferative and antitumorogenic activity. Novel approaches to hybridization techniques were highlighted for augmenting the efficacy of the DHMP scaffold derivatives. The structure–activity relationships (SARs) of certain potent DHMP scaffold derivatives are discussed as well. Studies presented in this chapter may assist scientists in drug design and further development of novel DHMP entities that may prove not only much better, efficacious, and safer agents but also affordable. The plausible function of mitochondrial ROS in cancer prevention is also documented.