New 1,2,4-triazole-Chalcone hybrids induce Caspase-3 dependent apoptosis in A549 human lung adenocarcinoma cells

Ahmed, Fatma F.; El-Hafeez, Amer Ali Abd; Abbas, Samar H.; Abdelhamid, Dalia; Abdel‐Aziz, Mohamed

doi:10.1016/j.ejmech.2018.03.073

Cited by 64 publications

(46 citation statements)

References 61 publications

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“…Every year, 1.2 million people are diagnosed with CRC [1][2][3][4]. Evasion of apoptosis is one of the hallmarks of cancer, in general, and correlated to drug resistance and metastatic spread, which urges the development of new drugs [5][6][7]. Apoptosis occurs through the extrinsic pathway or intrinsic pathway.…”

Section: Introductionmentioning

confidence: 99%

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Effect of Oxaliplatin-Loaded Poly (d,l-Lactide-co-Glycolic Acid) (PLGA) Nanoparticles Combined with Retinoic Acid and Cholesterol on Apoptosis, Drug Resistance, and Metastasis Factors of Colorectal Cancer

et al. 2020

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Apoptosis signaling pathways, drug resistance, and metastasis are important targets to develop new cancer treatments. We developed cholesterol-coated Poly(d,l-Lactide-co-Glycolic Acid) (PLGA) nanoparticles for effective encapsulation and delivery of retinoic acid and oxaliplatin to analyze their antitumor activity in colorectal cancer. The cell viability and proliferation of tumoral cells lines (CT-26 and SW-480) decreased when compared to control in vitro after treatment with the nanoparticles. In addition, apoptosis of CT-26 cells increased. Importantly, cytoprotection of nontumor cells was detected. Expression of pro-apoptotic proteins was upregulated, while anti-apoptotic proteins were downregulated either in vitro or in vivo. In addition, drug resistance and metastasis factors were downregulated in vivo. Human colorectal tumors that highly expressed BCL-2 and Ki-67 had a greater tendency towards death within 60 months. Our results show that loading oxaliplatin combined with retinoic acid and cholesterol in a nanoparticle formulation enables determination of optimal antitumor activity and subsequent treatment efficacy.

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Section: Introductionmentioning

confidence: 99%

“…Apoptosis occurs through the extrinsic pathway or intrinsic pathway. Both pathways converge at the activation of caspase-3, which then induces other caspases downstream of caspase-3 and eventually leads to apoptosis of the cancer cells [6,8].…”

Section: Introductionmentioning

confidence: 99%

Effect of Oxaliplatin-Loaded Poly (d,l-Lactide-co-Glycolic Acid) (PLGA) Nanoparticles Combined with Retinoic Acid and Cholesterol on Apoptosis, Drug Resistance, and Metastasis Factors of Colorectal Cancer

et al. 2020

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“…Thus, both chloro-and dimethylamino-derivatives of compound X (Figure 1), showed cytotoxic activity against human leukaemia cells with CC 50 ¼2.17 and 2.06 lM, respectively 40 . While, compound XI ( Figure 1) was apoptosis inducer in A549 cells 45 .…”

Section: Introductionmentioning

confidence: 90%

2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors

Lamie

Philoppes

2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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A novel 2-thiopyrimidine/chalcone hybrid was designed, synthesised, and evaluated for their cytotoxic activities against three different cell lines, K-562, MCF-7, and HT-29. The most active cytotoxic derivatives were 9d, 9f, 9n, and 9p (IC 50 ¼0.77-1.74 mM, against K-562 cell line), 9a and 9r (IC 50 ¼1.37-3.56 mM against MCF-7 cell line), and 9a, 9l, and 9n (IC 50 ¼2.10 and 2.37 mM against HT-29 cell line). Compounds 9a, 9d, 9f, 9n, and 9r were further evaluated for their cytotoxicity against normal fibroblast cell line WI38. Moreover, STAT3 and STAT5a inhibitory activities were determined for the most active derivatives 9a, 9d, 9f, 9n, and 9r. Dual inhibitory activity was observed in compound 9n (IC 50 ¼113.31 and 50.75 mM, against STAT3 and STAT5a, respectively). Prediction of physicochemical properties, drug likeness score, pharmacokinetic and toxic properties was detected.

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“…Ahmed et al designed new 1,2,4‐triazole‐chalcone hybrids ( 33 , 34 ) (Figure ) and tested them for anticancer activity. Their results revealed that compounds 33q , 33r , 33t , 34n, and 34t showed the highest cytotoxicity against human lung adenocarcinoma A549 cells (IC 50 = 4.4–16.04).…”

Section: Pharmacological Applications Of 124‐triazolementioning

confidence: 99%

Exploring recent developments on 1,2,4‐triazole: Synthesis and biological applications

Sathyanarayana

Poojary

2020

J Chinese Chemical Soc

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Triazoles are nitrogen-bearing heterocycles. In the last few decades, researchers have focused on fused heterocycles, as they have better pharmacological effect compared to triazoles alone. Among the two isomers of triazole, this article aims to explore the work carried out on 1,2,4-triazole and N-bridged heterocycles derived from 1,2,4-triazole in last 18 years, highlight different synthetic pathways, and present a brief summary of the different biological activities possessed by 1,2,4-triazole derivatives. The information collected in this article is expected to help researchers to discover novel therapeutic agents for better applications in the field of pharmaceutical science. K E Y W O R D Sbio-organic chemistry, medicinal chemistry, organic chemistry

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New 1,2,4-triazole-Chalcone hybrids induce Caspase-3 dependent apoptosis in A549 human lung adenocarcinoma cells

Cited by 64 publications

References 61 publications

Effect of Oxaliplatin-Loaded Poly (d,l-Lactide-co-Glycolic Acid) (PLGA) Nanoparticles Combined with Retinoic Acid and Cholesterol on Apoptosis, Drug Resistance, and Metastasis Factors of Colorectal Cancer

Effect of Oxaliplatin-Loaded Poly (d,l-Lactide-co-Glycolic Acid) (PLGA) Nanoparticles Combined with Retinoic Acid and Cholesterol on Apoptosis, Drug Resistance, and Metastasis Factors of Colorectal Cancer

2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors

Exploring recent developments on 1,2,4‐triazole: Synthesis and biological applications

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