Photo-induced synthesis of Axinastatin 3 analogs, the secondary structures and their in vitro antitumor activities

Photoinduced Synthesis of Methylated Marine Cyclopeptide Galaxamide Analogs with Isoindolinone as Anticancer Agents

“…The synthesis of linear peptides is similar to our previous report [37]. Generally, N-Boc-amino acid (10 mmol) was used as the starting material, N-benzyl-1-(trimethylsilyl)-methanamine (1 equivalent, 10 mmol) was used as a masking agent for the carboxyl end group, 2-ethoxy-1-ethoxycarbonyl-1,2-dihydroquinoline (EEDQ) (1.5 molar equivalents, 15 mmol in 10 mL of THF) was used as a condensing agent, and trifluoroacetic acid (TFA) (3 molar equivalents) was used as a deprotecting agent to prepare the N-benzyl-1-(trimethylsilyl)-methanamine-substituted linear peptides (Scheme 1).…”

Photo-induced synthesis and antitumor activity of marine zygosporamide analogs containing the isoindolinone fragment

“…Based on our previous studies, it can be observed that the different conformations of the cyclic peptide with isoindolinone presented disparate antitumor activities. 15,16 In this paper, we performed MTT assays on compounds 8 and 9 prepared against HepG-2 cells in parallel, and checked their cell morphologies using a fluorescence inverted microscope (FIM). The IC 50 value of compound 9 against HepG-2 cells was 22.37 AE 0.72 mg mL À1 , which was not as satisfactory as the corresponding value of compound 8 (12.08 AE 0.50 mg mL À1 ), but it still displayed a moderate ability to inhibit tumor growth.…”