Synthesis and in vitro antitumor activity of new quinoxaline derivatives.
A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines has been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of human cancers. Some of these compounds exhibited inhibitory effects on the growth of a wide range of cancer cell lines generally at 10(-6) M, in some cases at 10(-7) M and 10(-8) M concentrations. Within this series the benzylamino quinoxaline derivatives 1b-7b were the most active, whereas compound 2c showed the highest MG_MD value (-5.66).
Corona
Paola
P
Dipartimento Farmaco Chimico Tossicologico, Università degli Studi di Sassari, Via Muroni 23/A, 07100 Sassari, Italy. pcorona@uniss.it
Carta
Antonio
A
Loriga
Mario
M
Vitale
Gabriella
G
Paglietti
Giuseppe
G
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D011810:Quinoxalines