Design, synthesis and biological evaluation of novel α-hederagenin derivatives with anticancer activity

被引：19
|
作者：
Liu, Xian-xuan [1 ]
Yang, Yan-ting [1 ]
Wang, Xiao [1 ]
Wang, Kai-yi [1 ]
Liu, Jia-qi [1 ]
Lei, Lei [1 ,2 ,3 ]
Luo, Xiao-min [4 ]
Zhai, Rong [1 ]
Fu, Feng-hua [1 ]
Wang, Hong-bo [1 ]
Bi, Yi [1 ,4 ]
机构：
[1] Yantai Univ, Key Lab Mol Pharmacol & Drug Evaluat, Collaborat Innovat Ctr Adv Drug Delivery Syst & B, Sch Pharm,Minist Educ, Yantai 264005, Peoples R China
[2] Chinese Acad Med Sci, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China
[3] Peking Union Med Coll, Beijing 100050, Peoples R China
[4] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2017年 / 141卷
关键词：
alpha-Hederagenin derivatives; Synthesis; Apoptosis; Cancer; CYTOTOXIC ACTIVITY; APOPTOSIS; ACID; CARCINOGENESIS; MITOCHONDRIA;
D O I：
10.1016/j.ejmech.2017.09.016
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In an attempt to arrive at a more potent cytotoxic agent than the parent compound a-hederagenin (H), 24 alpha-hederagenin derivatives (5-8,11-24, 27-28, 31-32, and 35-36) were synthesized in a concise and efficient strategy and screened for in vitro cytotoxicity against the human cancer cell lines MKN45 and KB. Among these compounds, the polyamine derivative 15 exhibited more potency than the parent compound with IC50 values in the range of 4.22 AM-8.05 mu M. Compound 15 increased Baxibc1-2 ratio that disrupted the mitochondrial potential and induced apoptosis. Therefore, the present studies highlight the importance of polyamine derivatives of alpha-hederagenin in the discovery and development of novel anticancer agents. (C) 2017 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：427 / 439
页数：13
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