Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines
Само за регистроване кориснике
2014
Чланак у часопису (Објављена верзија)
,
Springer
Метаподаци
Приказ свих података о документуАпстракт
Antiproliferative activity of twenty one Michael adducts of aroylacrylic acids and cyclic amines ( N -Me-piperazine, imidazole, 2-Me-imidazole, and indole) was tested toward five human tumor cell lines (HeLa, LS174, K562, FemX, MDA-MB-361) in vitro. Compounds exerted antiproliferative activity in the high to the single-digit micromolar concentrations, causing increase of the cell population fraction in S phase and apoptosis. N -Me-piperazine and imidazole derivatives of aroylacrylic acids substituted with bulky alkyl substituents (2,4-di- i -Pr-Ph-, 2,4,6-tri-Et-Ph-, or β -tetrahydronaphthyl-) showed the best potency, while indole adducts were proved as the inferior antiproliferative agents. Few compounds showed significant selectivity, tumor versus healthy cells, with selectivity index ∼60 for the most selective congener. An unbiased in silico distinction between more and less potent compounds was obtained from 3D QSAR models derived by alignment-independent GRIND-2 descripto...rs.
Кључне речи:
Antiproliferative activity / Selectivity / Michael adducts / Aroylacrylic acids / 3D QSARИзвор:
Molecular Diversity, 2014, 18, 3, 577-592Издавач:
- Springer
Финансирање / пројекти:
DOI: 10.1007/s11030-014-9528-4
ISSN: 1381-1991
PubMed: 24874228
WoS: 000338641700009
Scopus: 2-s2.0-84903818978
Институција/група
IHTMTY - JOUR AU - Juranić, Ivan AU - Tošić, Ana V. AU - Kolundžija, Branka AU - Drakulić, Branko PY - 2014 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/2670 AB - Antiproliferative activity of twenty one Michael adducts of aroylacrylic acids and cyclic amines ( N -Me-piperazine, imidazole, 2-Me-imidazole, and indole) was tested toward five human tumor cell lines (HeLa, LS174, K562, FemX, MDA-MB-361) in vitro. Compounds exerted antiproliferative activity in the high to the single-digit micromolar concentrations, causing increase of the cell population fraction in S phase and apoptosis. N -Me-piperazine and imidazole derivatives of aroylacrylic acids substituted with bulky alkyl substituents (2,4-di- i -Pr-Ph-, 2,4,6-tri-Et-Ph-, or β -tetrahydronaphthyl-) showed the best potency, while indole adducts were proved as the inferior antiproliferative agents. Few compounds showed significant selectivity, tumor versus healthy cells, with selectivity index ∼60 for the most selective congener. An unbiased in silico distinction between more and less potent compounds was obtained from 3D QSAR models derived by alignment-independent GRIND-2 descriptors. PB - Springer T2 - Molecular Diversity T1 - Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines VL - 18 IS - 3 SP - 577 EP - 592 DO - 10.1007/s11030-014-9528-4 ER -
@article{ author = "Juranić, Ivan and Tošić, Ana V. and Kolundžija, Branka and Drakulić, Branko", year = "2014", abstract = "Antiproliferative activity of twenty one Michael adducts of aroylacrylic acids and cyclic amines ( N -Me-piperazine, imidazole, 2-Me-imidazole, and indole) was tested toward five human tumor cell lines (HeLa, LS174, K562, FemX, MDA-MB-361) in vitro. Compounds exerted antiproliferative activity in the high to the single-digit micromolar concentrations, causing increase of the cell population fraction in S phase and apoptosis. N -Me-piperazine and imidazole derivatives of aroylacrylic acids substituted with bulky alkyl substituents (2,4-di- i -Pr-Ph-, 2,4,6-tri-Et-Ph-, or β -tetrahydronaphthyl-) showed the best potency, while indole adducts were proved as the inferior antiproliferative agents. Few compounds showed significant selectivity, tumor versus healthy cells, with selectivity index ∼60 for the most selective congener. An unbiased in silico distinction between more and less potent compounds was obtained from 3D QSAR models derived by alignment-independent GRIND-2 descriptors.", publisher = "Springer", journal = "Molecular Diversity", title = "Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines", volume = "18", number = "3", pages = "577-592", doi = "10.1007/s11030-014-9528-4" }
Juranić, I., Tošić, A. V., Kolundžija, B.,& Drakulić, B.. (2014). Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines. in Molecular Diversity Springer., 18(3), 577-592. https://doi.org/10.1007/s11030-014-9528-4
Juranić I, Tošić AV, Kolundžija B, Drakulić B. Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines. in Molecular Diversity. 2014;18(3):577-592. doi:10.1007/s11030-014-9528-4 .
Juranić, Ivan, Tošić, Ana V., Kolundžija, Branka, Drakulić, Branko, "Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines" in Molecular Diversity, 18, no. 3 (2014):577-592, https://doi.org/10.1007/s11030-014-9528-4 . .