Synthesis and Antitumor Activity Evaluation of Novel Hsp90 Inhibitors(Ⅰ)

• 作 者: DiLiu;ChunwanLv;XiaoguangChen;XiaomingYu;
• 机 构: Institute of Materia Medica,Peking Union Medical College & Chinese Academy of Medical Sciences,No.1
• 出 处: 第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
• 发表日期: 2012年期

　　Heat shock protein 90 (Hsp90) is a recently recognized important target of cancer chemotherapy.Nearly 20 small molecule Hsp90 inhibitors are currently under clinical trails for their potential in treatment of cancer.A series of novel [1,2,3]triazolo[1,5-a]pyrazine Hsp90 inhibitors were discovered in our laboratory.These compounds were easily prepared by utilizing an intramolecular dipolar cycloaddition reaction,and showed significant anticancer activities in vitro (IC50 1-10μM) and in vivo as well.