6901-87-7

Upstream product

• 26061-06-3 methyl 2-((2S)-2-((tert-butoxycarbonyl)amino)propanamido)acetate 
• 62437-31-4 L-alanylglycine methyl ester trifluoroacetate 
• 123-08-0 4-hydroxy-benzaldehyde 
• 6138-90-5 trans-geranyl bromide 
• 62299-38-1 4-{[(2E)-3,7-dimethylocta-2,6-dien-1-yl]oxy}benzaldehyde 
• 74124-56-4 (3S)-1,4-diacetyl-3-methylpiperazine-2,5-dione 
• 4526-77-6 (S)-3-methyl-2,5-piperazinedione 
• 106-24-1 Geraniol 

Relevant academic research and scientific papers

Synthesis and anti-cancer activity of naturally occurring 2,5-diketopiperazines

Three naturally occurring oxyprenylated diketopiperazines were synthesized and preliminarily tested as growth inhibitory agents in vitro against various cancer cell lines. The compounds were tested on six human cancer cell lines with different sensitivity to proapoptotic stimuli using the MTT colorimetric assay. The data revealed that of the chemicals under study only deoxymicelianamide (11) displayed the highest activity, recording mean IC50 growth inhibitory values ranging from 2 to 23 μM. A comparative study with the non-geranylated saturated derivative of (11) revealed the importance of the presence of the geranyloxy side chain and the exocyclic 2,5-DPK double bond moiety for the observed activity.

Synthesis and bioactivity of diketopiperazine PJ147 and its derivatives from Gliocladium sp. YUP08

Concise total synthesis of diketopiperazine PJ147, obtained from mycelium of Gliocladium sp. YUP08, has been achieved in seven steps with 43.5% overall yield. Biological evaluation of PJ147 exhibited strong inhibiting activity against A375-S2, Hela, P388, A-549, HL-60, and BEL-7420 cell lines. Thus, eight derivatives of PJ147 with high water solubility were also synthesized to facilitate the in vivo bioassay of this kind of diketopiperazines. 2014