New mustard-linked 2-aryl-bis-benzimidazoles with anti-proliferative activity.
We describe new methodology for the synthesis of symmetric bis-benzimidazoles carrying 2-aryl moieties, including 2-[4-(3'-aminopropoxy)phenyl] and 2-[4-(3'-aminopropanamido)phenyl] substituents, together with the synthesis of novel hybrid molecules comprising bis-benzimidazoles in ester and amide combination with the N-mustard chlorambucil. The in vitro activities of these compounds against five cancer cell lines are also provided.
School of Chemistry, Queen's University Belfast, Stranmillis Road, Belfast, UK BT9 5AG.
Christine
C
Le Sann
Anne
A
Baron
John
J
Mann
Hendrik
H
van den Berg
Mekala
M
Gunaratnam
Stephen
S
Neidle
D000577:Amides; D020029:Base Pairing; D001483:Base Sequence; D001547:Benzaldehydes / Q000737:chemistry; D001562:Benzimidazoles / Q000737:chemistry* / Q000633:toxicity*; D002455:Cell Division / Q000187:drug effects*; D045744:Cell Line, Tumor; D002699:Chlorambucil / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004273:DNA, Neoplasm / Q000737:chemistry / Q000187:drug effects; D004952:Esters; D006801:Humans; D008466:Mechlorethamine / Q000737:chemistry* / Q000633:toxicity; D008958:Models, Molecular; D008968:Molecular Conformation; D009838:Oligodeoxyribonucleotides / Q000737:chemistry; D011759:Pyrrolidines / Q000737:chemistry; D012235:Rhodamines
D000577:Amides; D001547:Benzaldehydes; D001562:Benzimidazoles; D004273:DNA, Neoplasm; D004952:Esters; D009838:Oligodeoxyribonucleotides; D011759:Pyrrolidines; D012235:Rhodamines; D002699:Chlorambucil; D008466:Mechlorethamine; C032175:benzaldehyde