Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents

Synthesis and Evaluation of Millepachine Amino Acid Prodrugs With Enhanced Solubility as Antitumor Agents

“…On the other hand, 7a was demonstrated to exhibit a feature of long‐term restraint on cell viability. It was also revealed that 7a maintained the antitubulin property as like reported in other series of MIL derivatives . The ability to disrupt microtubules could be a bonus to the value of 7a , for this class of agents still stand as the best for cancer chemotherapy .…”

“…By adding a 3′‐hydroxyl group on B ring, compound 6 was obtained (Figure ). 6 showed improved antiproliferation activity compared to MIL in several tumor cell lines, and its derivatives generated by further modifying on the hydroxyl group were demonstrated with well antineoplastic potency in vitro and in vivo . These data suggested that 6 may be a promising lead compound.…”

SKLB316, a novel small-molecule inhibitor of cell-cycle progression, induces G2/M phase arrest and apoptosis in vitro and inhibits tumor growth in vivo

“…The current studies implicate that the effects of SKLB316 on G2/M cell cycle arrest and apoptosis might be via various direct and indirect pathways. Microtubules play critical rules in the mitotic spindle formation and dysregulation of its function will probably lead to the G2/M cell cycle arrest [23]. So we investigated whether microtubule is the target of SKLB316.…”

“…Images were then taken using an inverted fluorescence microscope (Olympus, Tokyo, Japan) after washing twice with PBS. Because the microtubules of HCT116 and CFPAC-1 cells are not easy to see in the fluorescence microscope, we chosen Hep G2 cells in this study as described previously [23]. Paclitaxel and colchicines served as positive controls.…”

“…The study was conducted as described previously with some modifications [23]. Cells (5000 cells/well) are seeded in Millicell EZ SLIDE 8 well glass slide (Millipore, Ireland) for 24 hours and then treated with different concentrations of SKLB316 (1, 2 and 4 μM) for 12 hours.…”