167316-06-5Relevant articles and documents
Synthesis and conformation studies of rubiyunnanin B analogs
Liu, Na-Na,Zhao, Si-Meng,Zhao, Jing-Feng,Zeng, Guang-Zhi,Tan, Ning-Hua,Liu, Jian-Ping
, p. 6630 - 6640 (2015/03/30)
Five new analogs 4-8 of rubiyunnanin B (1), mainly modified on the tetrapeptide subunit, were synthesized. These agents 4-8 were substituted d-Ala-l-Ala-l-Tyr(OMe)-l-Ala, d-Ala-l-Ala-l-Phe-l-Ala, d-Ala-l-Ala-l-Try-l-Ala, d-Ala-l-Ala-l-Pro-l-Ala, and d-Ala-l-Ala-l-Ala for the d-Ala-l-Ala-l-N-Me-Tyr(OMe)-l-Ala tetrapeptide subunit. Unlike the natural product, the synthetic agents 4-8 adopt only a single solution conformation, and the central peptide bond in the cyclodityrosine subunit of compounds 4-8 adopt trans stereochemistry. Cytotoxic activities of analogs 4-8 against three human cancer cell lines including A549, BGC-823, and HeLa were evaluated and all the five synthesized peptides exhibited no effects against the test cell lines. These compounds were also evaluated for their antiinsulin resistance and insulin sensitizing activities and none of them showed activity in these assays.
Linear TMC-95-based proteasome inhibitors
Basse, Nicolas,Piguel, Sandrine,Papapostolou, David,Ferrier-Berthelot, Alexandra,Richy, Nicolas,Pagano, Maurice,Sarthou, Pierre,Sobczak-Thépot, Jo?lle,Reboud-Ravaux, Michele,Vidal, Jo?lle
, p. 2842 - 2850 (2008/02/07)
We have designed and evaluated 45 linear analogues of the natural constrained cyclopeptide TMC-95A. These synthetically less demanding molecules are based on the tripeptide sequence Y-N-W of TMC-95A. Structural variations in the amino acid side chains and
Semisynthesis of an analogue of antitumor bicyclic hexapeptide RA-VII by fixing the Ala-2/Tyr-3 bond to cis by incorporating a triazole cis-amide bond surrogate
Hitotsuyanagi, Yukio,Motegi, Shuichi,Hasuda, Tomoyo,Takeya, Koichi
, p. 1111 - 1114 (2007/10/03)
We prepared an analogue of an antitumor bicyclic hexapeptide RA-VII whose amide configuration between residues 2 and 3 was fixed to cis by incorporating a triazole cis-amide bond surrogate. This analogue was shown, by NMR studies, to take almost the same