Sarli Vasiliki, Huemmer Stefan, Sunder-Plassmann Nils, Mayer Thomas U, Giannis Athanassios
University of Leipzig, Institute for Organic Chemistry, Johannisallee 29, 04103, Leipzig, Germany.
Chembiochem. 2005 Nov;6(11):2005-13. doi: 10.1002/cbic.200500168.
Human Eg5 is a mitotic kinesin that is essential for bipolar spindle formation and maintenance during mitosis. Recently, the discovery of compounds that inhibit Eg5 and cause mitotic arrest has attracted great interest, due to their potential use as the next generation of antimitotics. Here, we present the synthesis and biological investigation of 3,4-dihydrophenylquinazoline-2(1H)-thiones as selective and potent Eg5 inhibitors.
人驱动蛋白Eg5是一种有丝分裂驱动蛋白，在有丝分裂过程中对双极纺锤体的形成和维持至关重要。最近，由于其作为下一代抗有丝分裂药物的潜在用途，能够抑制Eg5并导致有丝分裂停滞的化合物的发现引起了极大关注。在此，我们报道了3,4-二氢苯基喹唑啉-2(1H)-硫酮作为选择性强效Eg5抑制剂的合成及生物学研究。
