TY - JOUR
T1 - Structure-Activity Relationships of Pyrrole Amidine Antiviral Antibiotics. 1. Modifications of the Alkylamidine Side Chain
AU - Bialer, Meir
AU - Yagen, Boris
AU - Mechoulam, Raphael
AU - Becker, Yechiel
PY - 1979/2/1
Y1 - 1979/2/1
N2 - Representatives of three types of side-chain analogues of distamycin A (1) were synthesized. These were tested for cytotoxicity, inhibition of herpes simplex virus (HSV) replication in cultured cells, effects on the synthesis of HSV DNA in isolated nuclei in vitro, as well as on DNA synthesis by purified HSV DNA polymerase. Distamycin A was the most active compound in all three antiviral tests, as well as the most toxic. However, several compounds, in particular the aromatic analogues 15 and 16, showed no toxicity under the experimental conditions used but were still very active in the three antiviral tests.
AB - Representatives of three types of side-chain analogues of distamycin A (1) were synthesized. These were tested for cytotoxicity, inhibition of herpes simplex virus (HSV) replication in cultured cells, effects on the synthesis of HSV DNA in isolated nuclei in vitro, as well as on DNA synthesis by purified HSV DNA polymerase. Distamycin A was the most active compound in all three antiviral tests, as well as the most toxic. However, several compounds, in particular the aromatic analogues 15 and 16, showed no toxicity under the experimental conditions used but were still very active in the three antiviral tests.
UR - http://www.scopus.com/inward/record.url?scp=0018639797&partnerID=8YFLogxK
U2 - 10.1021/jm00197a004
DO - 10.1021/jm00197a004
M3 - ???researchoutput.researchoutputtypes.contributiontojournal.article???
C2 - 230350
AN - SCOPUS:0018639797
SN - 0022-2623
VL - 22
SP - 1296
EP - 1301
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 11
ER -
