Selective anticancer activity of the novel thiobenzanilide 63T against human lung adenocarcinoma cells

Kucińska, Małgorzata; Piotrowska‐Kempisty, Hanna; Lisiak, Natalia; Kaczmarek, Mariusz; Dams‐Kozlowska, Hanna; Granig, Walter H.; Höferl, Martina; Jäger, Walter; Zehl, Martin; Murias, Marek; Erker, Thomas

doi:10.1016/j.tiv.2016.09.017

Cited by 4 publications

(9 citation statements)

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“…Moreover, experiments using the normal human fibroblast (CCD39Lu) and cancer cell lines confirmed the selective cytotoxic effect of 63 T. The calculated selectivity index after 48 h was 2.7 (IC 50 CCD39Lu/IC 50 A549), which is superior to results obtained in similar experiments for clinically approved drugs [25]. Our previous data showed that 63 T selectively induces cancer cell death in the caspase independent pathway, and the autophagic dose-dependent processes may be involved in the mechanism of cell death [25]. However, various aspects related to molecular targets and the antitumor effects of 63 T are still unknown [25].…”

Section: Introductionmentioning

confidence: 88%

“…To date, molecules built on benzanilide and thiobenzanilide scaffolds have been found to exert promising spasmolytic [19], antibacterial [20], antimycotic [21], antifungal [22] and estrogenic [23], as well anticancer [24, 25], activity. In previous studies, the cytotoxic activity of the thiobenzanilide derivative N,N′-(1,2-phenylene)bis3,4,5–trifluorobenzothioamide (63 T) has been broadly reviewed for a variety of cancer cell lines including breast and lung cancer [23].…”

Section: Introductionmentioning

confidence: 99%

“…In previous studies, the cytotoxic activity of the thiobenzanilide derivative N,N′-(1,2-phenylene)bis3,4,5–trifluorobenzothioamide (63 T) has been broadly reviewed for a variety of cancer cell lines including breast and lung cancer [23]. Particularly noteworthy is that 63 T exhibited significant anticancer activity against the lung cancer cell line A549 with a half maximal inhibitory concentration (IC 50 ) of >1 μM, 0.41 μM and 0.36 μM after 24 h, 48 h and 72 h, respectively [25]. Moreover, experiments using the normal human fibroblast (CCD39Lu) and cancer cell lines confirmed the selective cytotoxic effect of 63 T. The calculated selectivity index after 48 h was 2.7 (IC 50 CCD39Lu/IC 50 A549), which is superior to results obtained in similar experiments for clinically approved drugs [25].…”

Section: Introductionmentioning

confidence: 99%

“…Particularly noteworthy is that 63 T exhibited significant anticancer activity against the lung cancer cell line A549 with a half maximal inhibitory concentration (IC 50 ) of >1 μM, 0.41 μM and 0.36 μM after 24 h, 48 h and 72 h, respectively [25]. Moreover, experiments using the normal human fibroblast (CCD39Lu) and cancer cell lines confirmed the selective cytotoxic effect of 63 T. The calculated selectivity index after 48 h was 2.7 (IC 50 CCD39Lu/IC 50 A549), which is superior to results obtained in similar experiments for clinically approved drugs [25]. Our previous data showed that 63 T selectively induces cancer cell death in the caspase independent pathway, and the autophagic dose-dependent processes may be involved in the mechanism of cell death [25].…”

Section: Introductionmentioning

confidence: 99%

“…Our previous data showed that 63 T selectively induces cancer cell death in the caspase independent pathway, and the autophagic dose-dependent processes may be involved in the mechanism of cell death [25]. However, various aspects related to molecular targets and the antitumor effects of 63 T are still unknown [25]. In line with our preliminary studies, which indicated the generation of oxidative stress as a possible antitumor mechanism of 63 T, further experiments were designed to explore the anticancer effect of the aforementioned benzanilide derivative as an oxidative stress-inducing agent.…”

Section: Introductionmentioning

confidence: 99%

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The role of oxidative stress in 63 T-induced cytotoxicity against human lung cancer and normal lung fibroblast cell lines

et al. 2018

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SummaryIt has been shown previously that molecules built on benzanilide and thiobenzanilide scaffolds possess differential biological properties including selective anticancer activity. In our previous study, we examined the cytotoxic activity and mechanism of action of the thiobenzanilide derivative N,N′-(1,2-phenylene)bis3,4,5–trifluorobenzothioamide (63 T) as a potential chemotherapeutic compound in an experimental model employing A549 lung adenocarcinoma cells and CCD39Lu non-tumorigenic lung fibroblasts. Since the results suggested oxidative stress as a co-existing mechanism of the cytotoxic effect exerted by 63 T on tested cells, studies involving the analysis of reactive oxygen species (ROS) generation and markers of oxidative stress in cells incubated with 63 T were carried out. It may be concluded that the selective activity of 63 T against cancer cells shown in our experiments is caused, at least in part, by the response of the tested cells to 63 T mediated oxidative stress in both tested cell lines.Electronic supplementary materialThe online version of this article (10.1007/s10637-018-0704-8) contains supplementary material, which is available to authorized users.

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Section: Introductionmentioning

confidence: 88%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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The role of oxidative stress in 63 T-induced cytotoxicity against human lung cancer and normal lung fibroblast cell lines

et al. 2018

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Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives

Kurek

Myszkowski

Okulicz-Kozaryn

et al. 2021

Sci Rep

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Abstract10-Alkylthiocolchicines have been obtained and characterized by spectroscopic methods and their biological activities as: cytotoxic, anti-inflammatory and analgesic activities have been tested. Cytotoxic activity against SKOV-3 ovarian cell line for 10-alkylthiocolchicine analogues was reported and tested compounds showed to be more active than commonly used doxorubicin. Some of tested C-10 alkylthiolated colchicines have been found to exhibit cytotoxicity at levels comparable to that of the natural product—colchicine. 10-Methylthiocolchicine has IC50 = 8 nM and 10-ethylthiocolchicine has IC50 = 47 nM in comparison to colchicine IC50 = 37 nM. Moreover for 10-alkylthioderivatives apoptosis test, cyclin B1 and cell cycle tests were performed. 10-n-Butylthiocolchicine was tested for anti-inflammatory and analgesic activities it showed to produce analgesic rather than anti-inflammatory effect.

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More Than Resveratrol: New Insights into Stilbene-Based Compounds

et al. 2020

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The concept of a scaffold concerns many aspects at different steps on the drug development path. In medicinal chemistry, the choice of relevant “drug-likeness” scaffold is a starting point for the design of the structure dedicated to specific molecular targets. For many years, the chemical uniqueness of the stilbene structure has inspired scientists from different fields such as chemistry, biology, pharmacy, and medicine. In this review, we present the outstanding potential of the stilbene-based derivatives. Naturally occurring stilbenes, together with powerful synthetic chemistry possibilities, may offer an excellent approach for discovering new structures and identifying their therapeutic targets. With the development of scientific tools, sophisticated equipment, and a better understanding of the disease pathogenesis at the molecular level, the stilbene scaffold has moved innovation in science. This paper mainly focuses on the stilbene-based compounds beyond resveratrol, which are particularly attractive due to their biological activity. Given the “fresh outlook” about different stilbene-based compounds starting from stilbenoids with particular regard to isorhapontigenin and methoxy- and hydroxyl- analogues, the update about the combretastatins, and the very often overlooked and underestimated benzanilide analogues, we present a new story about this remarkable structure.

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Selective anticancer activity of the novel thiobenzanilide 63T against human lung adenocarcinoma cells

Cited by 4 publications

References 66 publications

The role of oxidative stress in 63 T-induced cytotoxicity against human lung cancer and normal lung fibroblast cell lines

The role of oxidative stress in 63 T-induced cytotoxicity against human lung cancer and normal lung fibroblast cell lines

Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives

More Than Resveratrol: New Insights into Stilbene-Based Compounds

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