Research output: Contribution to Journal/Magazine › Journal article › peer-review
Research output: Contribution to Journal/Magazine › Journal article › peer-review
}
TY - JOUR
T1 - Synthesis of bufalin derivatives with inhibitory activity against prostate cancer cells
AU - Yuan, Xiao-Feng
AU - Tian, Hai-Yan
AU - Li, Juan
AU - Jin, Lu
AU - Jiang, Shu-Tai
AU - Liu, Ken Wing-Keung
AU - Luo, Cheng
AU - Middleton, David A.
AU - Esmann, Mikael
AU - Ye, Wen-Cai
AU - Jiang, Ren-Wang
PY - 2014/6/3
Y1 - 2014/6/3
N2 - Bufalin possesses a strong anti-cancer effect, but the cardiac toxicity targeting the Na+, K+-ATPase limits its application. Here, two bufalin derivatives, bufadienolactam (1) and secobufalinamide (2), were synthesised by treating bufalin with ammonium acetate in dimethylformamide solution. Their structures were elucidated by extensive spectroscopic methods. The structure of compound 2 was further confirmed by single-crystal X-ray diffraction analysis. Compounds 1 and 2 expressed strong inhibitory activities against androgen-dependent prostate cancer cells (IC50 values about 10 mu M), but only weak inhibition on Na+, K+-ATPase (K-i about 70 mu M), indicating that they might be potential anti-prostate cancer agents without severe cardiac toxicity.
AB - Bufalin possesses a strong anti-cancer effect, but the cardiac toxicity targeting the Na+, K+-ATPase limits its application. Here, two bufalin derivatives, bufadienolactam (1) and secobufalinamide (2), were synthesised by treating bufalin with ammonium acetate in dimethylformamide solution. Their structures were elucidated by extensive spectroscopic methods. The structure of compound 2 was further confirmed by single-crystal X-ray diffraction analysis. Compounds 1 and 2 expressed strong inhibitory activities against androgen-dependent prostate cancer cells (IC50 values about 10 mu M), but only weak inhibition on Na+, K+-ATPase (K-i about 70 mu M), indicating that they might be potential anti-prostate cancer agents without severe cardiac toxicity.
KW - bufalin
KW - prostate cancer
KW - Na+
KW - K+-ATPase
KW - androgen receptor
KW - ANDROGEN-RECEPTOR-ANTAGONIST
KW - THERAPY
U2 - 10.1080/14786419.2014.881363
DO - 10.1080/14786419.2014.881363
M3 - Journal article
VL - 28
SP - 843
EP - 847
JO - Natural Product Research
JF - Natural Product Research
SN - 1478-6419
IS - 11
ER -