Liao, Lan-Shan; Tan, Lin-Jie; Chen, Yin; Yang, Qi-Yuan; Choudhary, Muhammad Iqbal; Pan, Ying-Ming; Tang, Hai-Tao; Su, Gui-Fa; Liang, Hong; Chen, Zhen-Feng published the artcile< One-pot synthesis of oxoaporphines as potent antitumor agents and investigation of their mechanisms of actions>, Reference of 721401-43-0, the main research area is oxoporphine derivative preparation antitumor agents; Antitumor activity; Apoptosis; Cell cycle; Oxoaporphine.
An efficient one-pot reaction for the synthesis of oxoaporphine alkaloids has been developed. Twenty-three compounds of oxoaporphine alkaloids were prepared and assessed for their antitumor activities. Most compounds inhibited the growth of T-24 tumor cells in vitro. Particularly, I displayed the most potent activity with an IC50 value of 0.5μM, which was 19-fold more potent than the parent compound 4. The substitution at C3-position of oxoaporphine core by -NO2 significantly enhanced the anticancer activity. Mechanism studies indicated that II and I induced cell cycle arrest at G2/M phase; in contrast, III induced cell cycle arrest at the S phase. Increase of mitochondrial ROS/Ca2+ and decrease of MMP, accompanied by activation of caspase-3/9, were observed in T-24 cells after exposure to compounds I, II and III, suggesting that the mitochondrial pathway was involved in the induced apoptosis. Moreover, compound I effectively inhibited tumor growth in a mouse xenograft model bearing T-24.
European Journal of Medicinal Chemistry published new progress about Alkaloids Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), BIOL (Biological Study), PREP (Preparation). 721401-43-0 belongs to class isoquinoline, and the molecular formula is C9H8BNO2, Reference of 721401-43-0.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem