Author(s): Krasavin Mikhail | Rufanov Konstantin | Sosnov Andrey | Karapetian Ruben | Godovykh Elena | Soldatkina Olga | Lavrovsky Yan | Gakh Andrei
Journal: Chemistry Central Journal
ISSN 1752-153X
Volume: 4;
Issue: 1;
Start page: 4;
Date: 2010;
Original page
ABSTRACT
Abstract A new chemical series of antiproliferative compounds was identified via high-throughput screening on DU-145 human prostate carcinoma cell line (hit compound potency - 5.7 μM). Exploration of the two peripheral diversity vectors of the hit molecule in a hit-targeted library and testing of the resulting compounds led to SAR generalizations and identification of the 'best' pharmacophoric moieties. The latter were merged in a single compound that exhibited a 200-fold better potency than the original hit compound. Specific cancer cell cytotoxicity was confirmed for the most potent compounds.
Journal: Chemistry Central Journal
ISSN 1752-153X
Volume: 4;
Issue: 1;
Start page: 4;
Date: 2010;
Original page
ABSTRACT
Abstract A new chemical series of antiproliferative compounds was identified via high-throughput screening on DU-145 human prostate carcinoma cell line (hit compound potency - 5.7 μM). Exploration of the two peripheral diversity vectors of the hit molecule in a hit-targeted library and testing of the resulting compounds led to SAR generalizations and identification of the 'best' pharmacophoric moieties. The latter were merged in a single compound that exhibited a 200-fold better potency than the original hit compound. Specific cancer cell cytotoxicity was confirmed for the most potent compounds.
