Description
NSC 5844 is a
bis-quinoline with diverse biological activities. It inhibits the growth of
P. falciparum strains that are sensitive (D-6) and resistant (W-2) to chloroquine
in vitro (IC
50s = 17 and 27 nM, respectively) but lacks activity against
P. berghei in vivo. NSC 5844 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with GI
50 values of 7.35 and 14.80 μM, respectively. It also inhibits 24% of botulinum neurotoxin serotype A light chain (BoNT/A LC) metalloprotease activity at a concentration of 20 μM.
Uses
N1,N2-Bis(7-chloroquinolin-4-yl)ethane-1,2-diamine and other bisquinoline derivatives have potentials against chloroquine-resistant malaria. A useful intermediate for the preparation of other antimalarial bisaminoquinlines.
References
[1] JONATHAN L. VENNERSTROM. Bisquinolines. 1. N,N-bis(7-chloroquinolin-4-yl)alkanediamines with potential against chloroquine-resistant malaria[J]. Journal of Medicinal Chemistry, 1992, 35 11: 2129-2134. DOI:
10.1021/jm00089a025[2] HAIWEN ZHANG . Synthesis and in vitro cytotoxicity evaluation of 4-aminoquinoline derivatives[J]. Biomedicine & Pharmacotherapy, 2008, 62 2: Pages 65-69. DOI:
10.1016/j.biopha.2007.04.007[3] JAMES C BURNETT . Novel small molecule inhibitors of botulinum neurotoxin A metalloprotease activity[J]. Biochemical and biophysical research communications, 2003, 310 1: Pages 84-93. DOI:
10.1016/j.bbrc.2003.08.112
