Standard

Privileged 1,2,4-oxadiazoles in anticancer drug design : Novel 5-aryloxymethyl-1,2,4-oxadiazole leads for prostate cancer therapy. / Lukin, Alexey; Karapetian, Ruben; Ivanenkov, Yan; Krasavin, Mikhail.

в: Letters in Drug Design and Discovery, Том 13, № 3, 01.03.2016, стр. 198-204.

Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование

Harvard

Lukin, A, Karapetian, R, Ivanenkov, Y & Krasavin, M 2016, 'Privileged 1,2,4-oxadiazoles in anticancer drug design: Novel 5-aryloxymethyl-1,2,4-oxadiazole leads for prostate cancer therapy', Letters in Drug Design and Discovery, Том. 13, № 3, стр. 198-204. https://doi.org/10.2174/1570180812999150812164251

APA

Lukin, A., Karapetian, R., Ivanenkov, Y., & Krasavin, M. (2016). Privileged 1,2,4-oxadiazoles in anticancer drug design: Novel 5-aryloxymethyl-1,2,4-oxadiazole leads for prostate cancer therapy. Letters in Drug Design and Discovery, 13(3), 198-204. https://doi.org/10.2174/1570180812999150812164251

Vancouver

Lukin A, Karapetian R, Ivanenkov Y, Krasavin M. Privileged 1,2,4-oxadiazoles in anticancer drug design: Novel 5-aryloxymethyl-1,2,4-oxadiazole leads for prostate cancer therapy. Letters in Drug Design and Discovery. 2016 Март 1;13(3):198-204. https://doi.org/10.2174/1570180812999150812164251

Author

Lukin, Alexey ; Karapetian, Ruben ; Ivanenkov, Yan ; Krasavin, Mikhail. / Privileged 1,2,4-oxadiazoles in anticancer drug design : Novel 5-aryloxymethyl-1,2,4-oxadiazole leads for prostate cancer therapy. в: Letters in Drug Design and Discovery. 2016 ; Том 13, № 3. стр. 198-204.

BibTeX

@article{cdae053722ec4a0f97ad1cce00f9f572,
title = "Privileged 1,2,4-oxadiazoles in anticancer drug design: Novel 5-aryloxymethyl-1,2,4-oxadiazole leads for prostate cancer therapy",
abstract = "Based on the structure of the previously identified leads, new series of compounds containing 1,2,4-oxadiazole core was designed. A small, diverse library of 51 compounds including both 2-(acylamino)ethyl and 2-ureidoethyl side chains was synthesized using parallel chemistry and tested for antiproliferative activity against prostate cancer DU-145 cell line. Four hit compounds - all belonging to 2-ureidoethyl series - were identified and three compounds were confirmed as 10-20 μM inhibitors. The similarity in compounds' periphery and the data obtained previously suggest a similar mode of action for these compounds which was postulated as tubulin inhibition and was confirmed by in silico docking. These data provide further evidence for the privileged character of 1,2,4-oxadiazoles in antiproliferative compound design.",
keywords = "1,2,4-oxadiazoles, Colchicines binding site, DU-145 cell line, Hit rate, In silico docking, Privileged structures, Prostate cancer, Tubulin inhibitors",
author = "Alexey Lukin and Ruben Karapetian and Yan Ivanenkov and Mikhail Krasavin",
year = "2016",
month = mar,
day = "1",
doi = "10.2174/1570180812999150812164251",
language = "English",
volume = "13",
pages = "198--204",
journal = "Letters in Drug Design and Discovery",
issn = "1570-1808",
publisher = "Bentham Science Publishers B.V.",
number = "3",

}

RIS

TY - JOUR

T1 - Privileged 1,2,4-oxadiazoles in anticancer drug design

T2 - Novel 5-aryloxymethyl-1,2,4-oxadiazole leads for prostate cancer therapy

AU - Lukin, Alexey

AU - Karapetian, Ruben

AU - Ivanenkov, Yan

AU - Krasavin, Mikhail

PY - 2016/3/1

Y1 - 2016/3/1

N2 - Based on the structure of the previously identified leads, new series of compounds containing 1,2,4-oxadiazole core was designed. A small, diverse library of 51 compounds including both 2-(acylamino)ethyl and 2-ureidoethyl side chains was synthesized using parallel chemistry and tested for antiproliferative activity against prostate cancer DU-145 cell line. Four hit compounds - all belonging to 2-ureidoethyl series - were identified and three compounds were confirmed as 10-20 μM inhibitors. The similarity in compounds' periphery and the data obtained previously suggest a similar mode of action for these compounds which was postulated as tubulin inhibition and was confirmed by in silico docking. These data provide further evidence for the privileged character of 1,2,4-oxadiazoles in antiproliferative compound design.

AB - Based on the structure of the previously identified leads, new series of compounds containing 1,2,4-oxadiazole core was designed. A small, diverse library of 51 compounds including both 2-(acylamino)ethyl and 2-ureidoethyl side chains was synthesized using parallel chemistry and tested for antiproliferative activity against prostate cancer DU-145 cell line. Four hit compounds - all belonging to 2-ureidoethyl series - were identified and three compounds were confirmed as 10-20 μM inhibitors. The similarity in compounds' periphery and the data obtained previously suggest a similar mode of action for these compounds which was postulated as tubulin inhibition and was confirmed by in silico docking. These data provide further evidence for the privileged character of 1,2,4-oxadiazoles in antiproliferative compound design.

KW - 1,2,4-oxadiazoles

KW - Colchicines binding site

KW - DU-145 cell line

KW - Hit rate

KW - In silico docking

KW - Privileged structures

KW - Prostate cancer

KW - Tubulin inhibitors

UR - http://www.scopus.com/inward/record.url?scp=84960107411&partnerID=8YFLogxK

U2 - 10.2174/1570180812999150812164251

DO - 10.2174/1570180812999150812164251

M3 - Article

AN - SCOPUS:84960107411

VL - 13

SP - 198

EP - 204

JO - Letters in Drug Design and Discovery

JF - Letters in Drug Design and Discovery

SN - 1570-1808

IS - 3

ER -

ID: 9716752