757967-72-9Relevant academic research and scientific papers
New cyclic somatostatin analogues containing a pyrazinone ring: Importance of Tyr for antiproliferative activity
Miyazaki, Anna,Tsuda, Yuko,Fukushima, Shoji,Yokoi, Toshio,Vantus, Tibor,Boekoenyi, Gyoengyi,Szabo, Edit,Horvath, Aniko,Keri, Gyoergy,Okada, Yoshio
scheme or table, p. 6199 - 6201 (2009/08/07)
Novel somatostatin analogues containing a pyrazinone ring, compounds 1 and 2, exhibited good antiproliferative activity on A431 tumor cells. To increase antitumor activity and binding affinity on somatostatin receptors (SSTRs), we substituted Tyr in the critical sequence, Tyr-d-Trp-Lys, with more hydrophobic aromatic residue. The substituted compounds dramatically lost antitumor activity, indicating that Tyr residue was an essential residue.
Design and synthesis of novel type somatostatin analogs with antiproliferative activities on A431 tumor cells
Miyazaki, Anna,Yokoi, Toshio,Tachibana, Yoshifumi,Enomoto, Riyo,Lee, Eibai,Bokonyi, Gyongyi,Keri, Gyorgy,Tsuda, Yuko,Okada, Yoshio
, p. 6323 - 6327 (2007/10/03)
It was reported that the somatostatin analog TT-232, d-Phe-c(Cys-Tyr-d-Trp- Lys-Cys)-Thr-NH2, exhibited a highly potent antitumor activity in vitro and in vivo. Using pyrazinone analogs and aliphatic amino acids instead of the disulfide bond, we prepared novel type somatostatin analogs including the sequence essential for antitumor activities, Tyr-d-Trp-Lys. These analogs exhibited antiproliferative effect on A431 tumor cells.
