757967-69-4Relevant academic research and scientific papers
Synthesis of somatostatin analogues containing C-terminal adamantane and their antiproliferative properties
Miyazaki, Anna,Tsuda, Yuko,Fukushima, Shoji,Yokoi, Toshio,Vántus, Tibor,B?k?nyi, Gy?ngyi,Szabó, Edit,Horváth, Anikó,Kéri, Gy?rgy,Okada, Yoshio
experimental part, p. 5121 - 5124 (2009/08/07)
On the basis of the structure of somatostatin analogue TT-232 (1), which exhibited a highly potent antitumor activity, we synthesized small linear peptide derivatives and evaluated their antitumor and apoptotic activity. Of them, Boc-Tyr-D-Trp-1-adamantylamide (5) had the most potent cell antiproliferative activity in SW480 and A431 cell lines, which was supported in A431 cell lines by FACS analysis that demonstrated a major increase in DNA fragmentation in the subG1 fraction.
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.
