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Parallel Synthesis of O ‐Phenoxyethyl and O ‐Adamantyl N‐ acyl Thiocarbamates Endowed with Antiproliferative Activity
Author(s) -
Spallarossa Andrea,
Cesarini Sara,
Sche Silvia,
Ranise Angelo
Publication year - 2009
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200800212
Subject(s) - chemistry , thiocarbamates , stereochemistry , mechanism of action , cell culture , biochemistry , biology , organic chemistry , in vitro , genetics
In order to further explore the antiproliferative properties of O ‐phenoxyethyl and O ‐adamantyl acylthiocarbamates (ATCs), a series of 14 derivatives was prepared by a parallel adaptation of a highly convergent one‐pot three‐step procedure. Ten acylthiocarbamates were selected by the National Cancer Institute drug evaluation program and screened against a panel of 55 to 58 cell lines derived from nine different types of human cancers. In general, the tested compounds showed a widespread micromolar activity with some specificity against leukemia, renal UO‐31, central nervous system (CNS) SNB‐75, and non‐small cell lung HOP‐92 cancer cell lines. Bioinformatic COMPARE analyses were carried out to identify possible mechanism(s) of action for acylthiocarbamate antiproliferative activity.