209983-91-5Relevant articles and documents
Synthesis of bengamide E analogues and their cytotoxic activity
Phi, Thi Dao,Mai, Huong Doan Thi,Tran, Van Hieu,Vu, Van Loi,Truong, Bich Ngan,Tran, Tuan Anh,Chau, Van Minh,Pham, Van Cuong
supporting information, p. 1830 - 1833 (2017/04/21)
A series of bengamide E analogues were prepared from the corresponding polyketide chain and amino acids via amide coupling reactions. Opening of the polyketide chain lactone ring with α-aminolactams was successfully achieved under microwave irradiation in the presence of sodium 2-ethyl hexanoate. A cytotoxic activity evaluation against a panel of cancer cell lines (KB, HepG-2, Lu-1, MCF-7, HL-60 and Hela) indicated that the 2′R analogues were generally more cytotoxic than the 2′S analogues. Additionally, several analogues exhibited selective inhibition against various cancer cell lines: compounds 32a and 32b selectively inhibited MCF-7 cells, while 33b and 35b were more sensitive toward Lu-1 and HepG-2, respectively. Notably, some of the synthetic analogues possess cytotoxic activities with IC50 values less than 1?μM.
Parallel liquid synthesis of N,N′-disubstituted 3-amino azepin-2-ones as potent and specific farnesyl transferase inhibitors
Le Diguarher, Thierry,Ortuno, Jean-Claude,Dorey, Gilbert,Shanks, David,Guilbaud, Nicolas,Pierre, Alain,Fauchere, Jean-Luc,Hickman, John A.,Tucker, Gordon C.,Casara, Patrick J.
, p. 3193 - 3204 (2007/10/03)
A rapid structure-activity study was performed by parallel liquid synthesis on N,N′-disubstitution of 3-amino azepin-2-one to afford potent and specific farnesyl transferase inhibitors with low nM enzymatic and cellular activities. The activities of the selected compounds were validated in vivo, and compounds 41a and 44a presented significant antitumour activity.