TY - JOUR
T1 - Substituted 2,5′-Bi-1H-benzimidazoles
T2 - Topoisoraerase I inhibition and cytotoxicity
AU - Kim, Jung Sun
AU - Gatto, Barbara
AU - Yu, Chiang
AU - Liu, Angela
AU - Liu, Leroy F.
AU - LaVoie, Edmond J.
PY - 1996/2/16
Y1 - 1996/2/16
N2 - Several 2′-aryl-5-substituted-2,5′-bi-1H-benzimidazole derivatives were synthesized and evaluated as topoisomerase I poisons and for their cytotoxicity toward the human lymphoblast cell line RPMI 8402. This study focused on 18 2,5′-bi-1H-benzimidazole derivatives which contained either a 5-cyano, a 5-(aminocarbonyl), or a 5-(4-methylpiperazinyl) group. Among these bibenzimidazoles, the pharmacological activity of 2′-phenyl derivatives and the influence of the different positional isomers of either a 2′-tolyl group or a 2′-naphthyl moiety on cytotoxicity and topoisomerase I inhibitory activity were determined.
AB - Several 2′-aryl-5-substituted-2,5′-bi-1H-benzimidazole derivatives were synthesized and evaluated as topoisomerase I poisons and for their cytotoxicity toward the human lymphoblast cell line RPMI 8402. This study focused on 18 2,5′-bi-1H-benzimidazole derivatives which contained either a 5-cyano, a 5-(aminocarbonyl), or a 5-(4-methylpiperazinyl) group. Among these bibenzimidazoles, the pharmacological activity of 2′-phenyl derivatives and the influence of the different positional isomers of either a 2′-tolyl group or a 2′-naphthyl moiety on cytotoxicity and topoisomerase I inhibitory activity were determined.
UR - http://www.scopus.com/inward/record.url?scp=0001325629&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0001325629&partnerID=8YFLogxK
U2 - https://doi.org/10.1021/jm950412w
DO - https://doi.org/10.1021/jm950412w
M3 - Article
C2 - 8632422
SN - 0022-2623
VL - 39
SP - 992
EP - 998
JO - Journal of medicinal chemistry
JF - Journal of medicinal chemistry
IS - 4
ER -