Entity

Time filter

Source Type


Trashin S.A.,Institute of Physiologically Active Compounds | Dubinina T.V.,Moscow State University | Fionov A.V.,Moscow State University | Tomilova L.G.,Moscow State University
Journal of Porphyrins and Phthalocyanines | Year: 2011

The electrochemical and spectroelectrochemical behavior of two planar binuclear naphthalocyanines containing benzene and naphthalene π-conjugated bridges was investigated for the first time. Their intense absorption in the near infrared region was observed even in a low polar solvent such as o-dichlorobenzene after electrochemical reduction at a potential of -0.4 V vs. SCE, which was not enough to reduce the complexes into their first reduction state. These data and EPR studies allow us to conclude that the electrochemically generated form is the true neutral form of the synthesized compounds whereas the suppression of the near-infrared bands is a result of the presence of their cation radicals as one-electron oxidized forms. © 2011 World Scientific Publishing Company.


Luzina E.L.,Institute of Physiologically Active Compounds | Popov A.V.,University of Pennsylvania
European Journal of Medicinal Chemistry | Year: 2010

A number of N-bis(trifluoromethyl)alkyl-N′-substituted ureas have been synthesized and evaluated for their in vitro anticancer activity against the human cancer cell lines at the National Cancer Institute (NCI, USA). Marked activity was shown for compounds 4a and 5a. The most sensitive cell lines relative to the tested compounds were: 4a UO-31 (renal cancer, log GI 50 -5.62), HS 578T (breast cancer, log GI50 -5.50), 5a HCC-2998 (colon cancer, log GI50 -5.94), NCI-H322M (lung cancer, log GI50 -5.75) and PC-3 (prostate cancer, log GI50 -5.66). © 2010 Elsevier Masson SAS. All rights reserved.


Luzina E.L.,Institute of Physiologically Active Compounds | Popov A.V.,University of Pennsylvania
Journal of Fluorine Chemistry | Year: 2014

Novel trifluoromethylated mono- and bicyclic succinimides derived from trifluoromethylmaleic anhydride were synthesized using cyclopentadiene or 2,3-dimethylbutadiene and (het)arylamines. The biological activity of these compounds was evaluated using prediction methods and experimental studies. This series of new trifluoromethyl succinimides (3a,b and 6a-c) were tested by the National Cancer Institute (NCI, Bethesda, USA) by Program NCI-60 DTP Human Tumor Cell Line Screen at a single high dose (10-5 M). Imides revealed activity on Leukemia cell lines (RPMI-8226 - myeloma cell line), Non-Small Cell Lung Cancer cell lines (A549/ATCC - lung carcinoma epithelial cells) and Renal cancer cell lines (A498 and SN12 C). © 2014 Elsevier B.V. All rights reserved.


Luzina E.L.,Institute of Physiologically Active Compounds | Popov A.V.,University of Pennsylvania
European Journal of Medicinal Chemistry | Year: 2012

A series of new synthesized N-bis(trifluoromethyl)alkyl-N'-substituted ureas have been tested in the National Cancer Institute (NCI, Bethesda, USA) by Program NCI-60 DTP Human Tumor Cell Line Screen at a single high dose (10 -5 M). COMPARE analysis has been carried out for all tested compounds. The tested compounds showed antitumor activity against individual cell lines. The most sensitive cell lines relative to the tested compounds are: 5g Leukemia RPMI-8226 (GI% 52.7), Non-Small Cell Lung cancer HOP-92 (GI % 88.53), NCI-H522 (GI % 64.41), Melanoma UACC-62 (GI% 53.08), SK-MEL-5 (GI % 74.63), Breast cancer MDA-MB-468 (GI% 51.29), T-47D (GI % 65.1), 5b Leukemia K-562 (GI % 55.55), 7m Leukemia HL-60(TB) (GI % 51.76). © 2012 Elsevier Masson SAS. All rights reserved.


Gakh A.A.,Oak Ridge National Laboratory | Gakh A.A.,University of Virginia | Sosnov A.V.,Institute of Physiologically Active Compounds | Krasavin M.,Griffith University | And 2 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

The combination of experimental (inhibition of colchicine binding) and computational (COMPARE, docking studies) data unequivocally identified diaryl 5-amino-1,2,4-oxadiazoles as potent tubulin inhibitors. Good correlation was observed between tubulin binding and cytostatic properties for all tested compounds with the notable exception of the lead candidate, 3-(3-methoxyphenyl)- 5-(4-methoxyphenyl)amino-1,2,4-oxadiazole (DCP 10500078). This compound was found to be substantially more active in our in vitro experiments than the monofluorinated title compound, 3-(2-fluorophenyl)-5-(4-methoxyphenyl)amino-1,2, 4-oxadiazole (DCP 10500067/NSC 757486), which in turn demonstrated slightly better tubulin binding activity. Comparative SAR analysis of 25 diaryl 5-amino-1,2,4-oxadiazoles with other known tubulin inhibitors, such as combretastatin A-4 (CA-4) and colchicine, provides further insight into the specifics of their binding as well as a plausible mechanism of action. © 2012 Elsevier Ltd. All rights reserved.

Discover hidden collaborations