Abstract
Kinesin is one of the microtubule-dependent motors which is essential for the cellular activities connected with microtubule, for instance cell division and intra-cellular transport. Kinesin spindle protein (KSP) or kinesin −5 is also shortly referred as Eg5, which is a member of kinesin family. During cell division of bipolar mitotic spindle, the kinesin Eg5 provides for its maintenance and formation. To hold anti-cancer action, block mitotic advancement and to weaken spindle assembly, tiny- molecule compound that inhibit Eg5 has a greater impact. In this study, to control mitotic kinesin Eg5, we have synthesized novel photochromic inhibitors which composed of photo-responsive azobenzene and Spiropyran derivatives and exhibit multiple photo isomers. This multiple isomerization states are crucial for clinical use and can control the therapy of the anticancer drugs more precisely. Previously, we synthetized the compound spiropyran-azobenzene-spiropyran, SP-AB-SP composed of two spiropyran derivatives and azobenzene derivative. SP-AB-SP was expected to change its structure and properties drastically accompanied by photoisomerizations. SP-AB-SP showed three photoisomerization states and the different inhibitory activities in the basal and MT dependent ATPase activity among the photoisomerization states. Currently, we synthesized the new inhibitor Spiropyran-Sulfonate Azobenzene, SP-Sulfo-AB. This compound also showed multiple isomerization states upon the Visible (VIS) light formed SP- Trans, UV light formed MC-Cis and SP- Cis and in the dark formed MC-Trans respectively. The synthesized compounds showed inhibitory activity of ATPase among their multiple isomerization states. The inhibitory effect of SP-Sulfo-AB for microtubules gliding on Eg5 was also examined. The inhibitor was applied in the Hela cell for observing the proliferation. Finally, the inhibitor showed antiproliferative activity in Hela cell.
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