Small molecule-mediated induction of endoplasmic reticulum stress in cancer cells

Abstract

Endoplasmic reticulum (ER) is one of the crucial sub-cellular organelles controlling myriads of functions including protein biosynthesis, folding, misfolding and unfolding. As a result, dysregulation of these pathways in ER...

Ionic liquids revolutionizing biomedicine: recent advances and emerging opportunities

“…66 Hydrazones, existing in chemotherapeutic agents and many other drugs, attached to organic molecules could be applied to drug design relevant to anticancer activities. [127][128][129] Al-Sodies et al designed and synthesized novel dicationic ILs (Di-ILs), which contained hydrazone as a spacer linking double pyridines with alkyl functionalized esters to form cations. In their experiment, the two most active Di-ILs showed 99.99% and 99.86% compromised cell ability against human lung cancer cells (A549 and H1299, respectively).…”

Small‐Molecule Endoplasmic Reticulum Stress Inducer Triggers Apoptosis in Cancer Cells

“…Subsequently, other small molecules to induce ER stress emerged as novel strategies towards next‐generation ER targeted cancer therapy [17–25] . However, development of ER targeted novel small molecules remained in its infancy due to the lack of proper targeting moieties [26–31] …”

“…[17][18][19][20][21][22][23][24][25] However, development of ER targeted novel small molecules remained in its infancy due to the lack of proper targeting moieties. [26][27][28][29][30][31] To address this, herein we have developed a library of 3-methoxy-pyrrole enamine derivatives having Dansyl or p-toluene sulfonyl (Tosyl) moieties for ER targeting (Figure 1a) through a concise three step chemical synthesis (Figure 1b). Through cell viability, confocal microscopy and gel electrophoresis studies we have identified a novel small molecule which homed into ER of the HeLa cervical cancer cells within 3 h followed by induction of ER stress leading to apoptosis to show remarkable HeLa cell killing (Figure 1d).…”