點擊化學及鈴木偶合反應方法建構鎖定DNA損害修復路徑之小分子雙效抑制劑

This proposal aims to construct mechanistically diverse dual inhibitory scaffolds that can target the DNA damage repair pathways and elicit amplified anticancer effects. Notably, the concept of addressing the DNA damage repair pathways via dual modulatory structural assemblages to exert antitumor effects is envisioned to overcome the limitations of DNA damage repair pathway inhibitors as their activity is selectively confined to tumors with BRCA mutations. This shortcoming places the tag of a narrow activity spectrum on such agents which hinders their therapeutic utility. In this context, a successful outcome of this proposal that aims to expand the activity spectrum of DNA damage repair pathway inhibitors via the strategy of concomitant/simultaneous inhibition of two targets can provide a new inception point to academicians/researchers/scientists working in this direction of research. To add on, budding and brightest science graduates can imbibe the skill of various scaffold construction approaches, lead modification approaches and biological profiling of bifunctional inhibitors. Overall, the long-run attempts are focused on extracting benefits through this research endeavour for the academicians, researchers, young scientists and the pharmaceutical industrial sector.