Antiviral Action of Benzo[de]isoquinoline–1,3–diones

Abstract

Two benzo[de]isoquinoline-diones, namely 5-nitro-2-(2-dimethylaminoethyl)-benzo[de]isoquinoline-1,3-dione and 5-nitro-2-[2-(1-pyrrolidine)-ethyl]-benzo[de]isoquino-line-1,3-dione, caused inhibition of the viral replication, when assayed against herpes simplex and vaccinia viruses in chick embryo cell cultures. Influenza and Sindbis virus replication were unaffected by these chemicals. Virucidal effects were unobserved. The inhibitory activity is time-related. Ocular and dermal infections with vaccinia virus in rabbits were prevented or disease severity reduced whenever they were treated with either one of these two drugs.

Phase II study of amonafide in advanced pancreatic adenocarcinoma

“…Using the human myeloid cell lines HL-60 and KBM-3, amonafide induced single strand breaks and topoisomerase-II mediated DNA cleavage, which disappeared rapidly following removal of the drug from the media [11][12][13]. In addition to these effects on DNA, amonafide has also been observed to inhibit protein and nucleotide synthesis at a concentration of 10 -5 M. At a concentration of 10-4 M, RNA and DNA synthesis was completely inhibited [15,16]. Preclinical activity of amonafide demonstrated a broad activity spectrum against 60% of the murine tumor cell lines [17,18].…”

Acetonide protection of dopamine for the synthesis of highly pure N-docosahexaenoyldopamine

“…Proper protection of the catechol group is often required during chemical modification of dopamine. Various catechol protecting groups have been reported, including methyl ether,7 cyclic ethyl orthoformate,8 t -butyldimethylsilyl,9 and acetonide 10. Easy protection/deprotection together with good stability to strong bases and weak acids makes the acetonide protective group especially useful 11.…”