Juan Feng, Yidong Liu, Xia Tian, Chen Shen, Zhiqiang Feng, Jingxu Zhang, Xiangli Yao, Meilin Pu, Xuguang Miao, Lan Ma, Shouxin Liu
Steroid hybrids have emerged as a type of advantageous compound as they could offer improved pharmacological and pharmaceutical properties. Here, we report a series of novel peptide-dehydroepiandrosterone hybrids, which would effectively induce endoplasmic reticulum stress (ERS) and lead to apoptosis with outstanding in vitro and in vivo anti-melanoma effects. The lead compound IId among various steroids conjugated with peptides and pyridines showed effective in vivo activity in B16 xenograft mice: in medium- and high-dose treatment groups (60 and 80 mg/kg), compound IId would significantly inhibit the growth of tumours by 98%-99% compared to the control group, with the highest survival rate as well...
March 7, 2024: European Journal of Medicinal Chemistry