53177-88-1Relevant articles and documents
Synthesis and cytotoxicity evaluation of 4′-amino-4′-dehydroxyloleandrin derivatives
Chen, Hu,Lei, Min,Ma, Biao,Liu, Miao,Guo, Dean,Liu, Xuan,Hu, Lihong
, p. 85 - 90 (2016)
A series of C4′-substituted oleandrin analogues were designed, synthesized and evaluated for their cytotoxicity towards human cervical carcinoma cell line (HeLa). The structure-activity relationships (SARs) of these compounds were summarized in this paper, and 4′-α-amino-4′-dehydroxyloleandrin 4a (IC50?=?21.7?nM) and 4′-β-amino-4′-dehydroxyloleandrin 4b (IC50?=?10.9?nM) exhibited stronger cytotoxicity compared with oleandrin (IC50?=?33.3?nM). Furthermore, the cytotoxicity of these two compounds towards another five human cancer cell lines (NCI-H266, A549, Jurkat, HL-60 and PC-3) was also evaluated and the IC50 values of β-amino derivative 4b were approximately 2–3 folds lower than that of oleandrin.
Synthesis of oleandrin derivatives and their cytotoxic activity
Chen, Xubing,Hou, Jinjun,Lei, Min,Long, Huali,Wu, Wanying,Zhang, Yanzhi,Zhang, Zijia,Zhou, Yang
, (2020/05/13)
A series of oleandrin-4′-yl ester derivatives were designed, synthesized, and evaluated for their proliferation inhibition activities against tumor cell lines. Cytotoxicity data revealed that the C4′ moiety had an important influence on cytotoxic activity. Several compounds that we designed and synthesized exhibit significant in vitro antiproliferative activity against the tested tumor cell lines. Among the derivatives of OL, 4b-HCl not only had good anti-tumor activity but also had good water solubility. Furthermore, 4b-HCl can significantly inhibit tumor growth by 96.4% at a dose of 6 mg/kg/d by ip.
