Synthesis, Molecular Structure, Anticancer Activity, and QSAR Study of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)Benzenesulfonamide Derivatives - Publikacja - MOST Wiedzy

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Synthesis, Molecular Structure, Anticancer Activity, and QSAR Study of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)Benzenesulfonamide Derivatives

Abstrakt

A series of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)benzenesulfonamides were synthesized from 4-amino-N-(aryl/heteroaryl)benzenesulfonamides and 2,5-dimethoxytetrahydrofuran. All the synthesized compounds were evaluated for their anticancer activity on HeLa, HCT-116, and MCF-7 human tumor cell lines. Compound 28, bearing 8-quinolinyl moiety, exhibited the most potent anticancer activity against the HCT-116, MCF-7, and HeLa cell lines, with IC50 values of 3, 5, and 7 M, respectively. The apoptotic potential of the most active compound (28) was analyzed through various assays: phosphatidylserine translocation, cell cycle distribution, and caspase activation. Compound 28 promoted cell cycle arrest in G2/M phase in cancer cells, induced caspase activity, and increased the population of apoptotic cells. Relationships between structure and biological activity were determined by the QSAR (quantitative structure activity relationships) method. Analysis of quantitative structure activity relationships allowed us to generate OPLS (Orthogonal Projections to Latent Structure) models with verified predictive ability that point out key molecular descriptors influencing benzenosulfonamide’s activity

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Beata Żołnowska, Jarosław Sławiński, Zdzisław Brzozowski, Anna Kawiak, Mariusz Belka, Joanna Zielińska, Tomasz Bączek, Jarosław Chojnacki. (2018). Synthesis, Molecular Structure, Anticancer Activity, and QSAR Study of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)Benzenesulfonamide Derivatives, 19(5), 1482-1505. https://doi.org/10.3390/ijms19051482

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Kategoria:
Publikacja w czasopiśmie
Typ:
artykuł w czasopiśmie wyróżnionym w JCR
Opublikowano w:
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES nr 19, wydanie 5, strony 1482 - 1505,
ISSN: 1422-0067
Język:
angielski
Rok wydania:
2018
Opis bibliograficzny:
Żołnowska B., Sławiński J., Brzozowski Z., Kawiak A., Belka M., Zielińska J., Bączek T., Chojnacki J.: Synthesis, Molecular Structure, Anticancer Activity, and QSAR Study of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)Benzenesulfonamide Derivatives// INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES. -Vol. 19, iss. 5 (2018), s.1482-1505

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