1097648-22-0Relevant 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.
