TY  - JOUR
AU  - Coskun, Goknil Pelin
AU  - Ozhan, Yagmur
AU  - Dobričić, Vladimir
AU  - Bošković, Jelena
AU  - Reis, Rengin
AU  - Sipahi, Hande
AU  - Sahin, Zafer
AU  - Demirayak, Seref
PY  - 2023
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4764
AB  - Cancer is the disease with the highest mortality. Drug studies contribute to promising treatments; however there is an urgent need for selective drug candidates. Pancreatic cancer is difficult to treat and the cancer progresses rapidly. Unfortunately, current treatments are ineffective. In this study, ten new diarylthiophene-2-carbohydrazide derivatives were synthesized and evaluated for their pharmacological activity. The 2D and 3D anticancer activity studies suggested the compounds 7a, 7d, and 7f were promising. Among these, 7f (4.86 µM) showed the best 2D inhibitory activity against PaCa-2 cells. Compounds 7a, 7d and 7f were also tested for their cytotoxic effects on healthy cell line but only compound 7d showed selectivity. Compounds 7a, 7d, and 7f showed the best 3D cell line inhibitory effect according to spheroid diameters. The compounds were screened for their COX-2 and 5-LOX inhibitory activity. For COX-2, the best IC50 value was observed for 7c (10.13 µM) and all compounds showed significantly lower inhibition compared to standard. In the 5-LOX inhibition study, compounds 7a (3.78 µM), 7c (2.60 µM), 7e (3.3 µM), and 7f (2.94 µM) demonstrated influential activity compared to standard. Regarding molecular docking studies, binding mode of compounds 7c, 7e, and 7f to the 5-LOX enzyme were non-redox or redox types, but not the iron-binding type. As dual inhibitors of 5-LOX and pancreatic cancer cell line, 7a and 7f were identified as the most promising compounds.
PB  - MDPI
T2  - Pharmaceutics
T1  - Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer
VL  - 15
IS  - 5
DO  - https://doi.org/10.3390/pharmaceutics15051441
ER  - 

@article{
author = "Coskun, Goknil Pelin and Ozhan, Yagmur and Dobričić, Vladimir and Bošković, Jelena and Reis, Rengin and Sipahi, Hande and Sahin, Zafer and Demirayak, Seref",
year = "2023",
abstract = "Cancer is the disease with the highest mortality. Drug studies contribute to promising treatments; however there is an urgent need for selective drug candidates. Pancreatic cancer is difficult to treat and the cancer progresses rapidly. Unfortunately, current treatments are ineffective. In this study, ten new diarylthiophene-2-carbohydrazide derivatives were synthesized and evaluated for their pharmacological activity. The 2D and 3D anticancer activity studies suggested the compounds 7a, 7d, and 7f were promising. Among these, 7f (4.86 µM) showed the best 2D inhibitory activity against PaCa-2 cells. Compounds 7a, 7d and 7f were also tested for their cytotoxic effects on healthy cell line but only compound 7d showed selectivity. Compounds 7a, 7d, and 7f showed the best 3D cell line inhibitory effect according to spheroid diameters. The compounds were screened for their COX-2 and 5-LOX inhibitory activity. For COX-2, the best IC50 value was observed for 7c (10.13 µM) and all compounds showed significantly lower inhibition compared to standard. In the 5-LOX inhibition study, compounds 7a (3.78 µM), 7c (2.60 µM), 7e (3.3 µM), and 7f (2.94 µM) demonstrated influential activity compared to standard. Regarding molecular docking studies, binding mode of compounds 7c, 7e, and 7f to the 5-LOX enzyme were non-redox or redox types, but not the iron-binding type. As dual inhibitors of 5-LOX and pancreatic cancer cell line, 7a and 7f were identified as the most promising compounds.",
publisher = "MDPI",
journal = "Pharmaceutics",
title = "Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer",
volume = "15",
number = "5",
doi = "https://doi.org/10.3390/pharmaceutics15051441"
}

Coskun, G. P., Ozhan, Y., Dobričić, V., Bošković, J., Reis, R., Sipahi, H., Sahin, Z.,& Demirayak, S.. (2023). Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer. in Pharmaceutics
MDPI., 15(5).
https://doi.org/https://doi.org/10.3390/pharmaceutics15051441

Coskun GP, Ozhan Y, Dobričić V, Bošković J, Reis R, Sipahi H, Sahin Z, Demirayak S. Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer. in Pharmaceutics. 2023;15(5).
doi:https://doi.org/10.3390/pharmaceutics15051441 .

Coskun, Goknil Pelin, Ozhan, Yagmur, Dobričić, Vladimir, Bošković, Jelena, Reis, Rengin, Sipahi, Hande, Sahin, Zafer, Demirayak, Seref, "Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer" in Pharmaceutics, 15, no. 5 (2023),
https://doi.org/https://doi.org/10.3390/pharmaceutics15051441 . .