1.
Bioorg Med Chem Lett
; 30(4): 126910, 2020 02 15.
Article
in English
| MEDLINE
| ID: mdl-31882300
ABSTRACT
Six N-nitroaryl-2-amino-1,3-dichloropropane derivatives have been prepared and evaluated against 18 cancer cell lines and two non-cancerous cell lines. Analysis of cell viability data and IC50 values indicated that the presence of a trifluoromethyl group in the nitroaryl moiety is an important structural feature associated with the compounds' cytotoxicities.
Subject(s)
Antineoplastic Agents/chemical synthesis , Propane/analogs & derivatives , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Line , Cell Survival/drug effects , Drug Screening Assays, Antitumor , Humans , Methylation , Prodrugs/chemical synthesis , Prodrugs/chemistry , Prodrugs/pharmacology , Propane/chemical synthesis , Propane/chemistry , Propane/pharmacology , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 26(24): 5851-5854, 2016 12 15.
Article
in English
| MEDLINE
| ID: mdl-27876476
ABSTRACT
A series of N-nitroarylated-3-chloromethyl-1,2,3,4-tetrahydroisoquinoline derivatives, several of which also possessed a trifluoromethyl substituent, were prepared and assessed as potential nitroaromatic prodrugs. The enzymatic reduction of these compounds and their cytotoxicities were studied. The compounds were cytotoxic, but this is probably not related to their enzymatic reduction.