Copyright (c) 2026 Srinivas Bandari Srinivas

This work is licensed under a Creative Commons Attribution 4.0 International License.
Design, Synthesis and Characterisation of New Trifluoroethyl Dihydroquinoxaline Carboxylate Amino Derivatives and Evaluation of their Biological Activities
Corresponding Author(s) : Ravinder Manchal
Asian Journal of Chemistry,
Vol. 38 No. 8 (2026): Vol 38, Issue 8 (2026)
Abstract
In this work, a series of novel 2,2,2-trifluoroethyl-1-methyl-2-oxo-1,2-dihydroquinoxaline-6-carboxylate amino derivatives (10a-v) was synthesised and their structures were confirmed by 1H NMR, IR and mass spectral analysis. The synthesised quinoxaline derivatives were screened for antibacterial and anticancer activity. The antibacterial activity results showed that derivatives 10c, 10e, 10f, 10h, 10n, 10o, 10p, 10t and 10u had excellent antibacterial activity against all the tested bacterial strains, namely Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis. The anticancer activity of the derivatives was evaluated against two human cancer cell lines, MCF-7 and HepG-2. The results showed that derivative 10m exhibits more potent activity compared to the standard drug erlotinib, while the remaining four compounds, 10i, 10j, 10k and 10l, show activity almost comparable to that of the standard drug. The molecular docking studies also support the in vitro anticancer activity results.
Keywords
Download Citation
Endnote/Zotero/Mendeley (RIS)BibTeX
- A.K. Sahoo and A. Bhattacharyya, Curr. Org. Chem., 28, 161 (2024); https://doi.org/10.2174/0113852728285439240109071659
- S. Tariq, K. Somakala and M. Amir, Eur. J. Med. Chem., 143, 542 (2018); https://doi.org/10.1016/j.ejmech.2017.11.064
- T. Fonseca, B. Gigante, M.M. Marques, T.L. Gilchrist and E. De Clercq, Bioorg. Med. Chem. Lett., 12, 103 (2004); https://doi.org/10.1016/j.bmc.2003.10.013
- H. Khatoon, Y. Rukayadi, S.M. Faudzi and Y. Rukayadi, ChemistrySelect, 9, e202305073 (2024); https://doi.org/10.1002/slct.202305073
- A. Elfadil, A.M. Alzahrani, H. Abdullah, H. Alsamhan, T.S. Abujamel, H.E. Ahmed and A. Jiman-Fatani, Infect. Drug Resist., 16, 2291 (2023); https://doi.org/10.2147/IDR.S401371
- K. Srinivas, P.V. Kumar, H. Joshi, A. Velidandi and R. Manchal, Russ. J. Bioorg. Chem., 49, 1068 (2023); https://doi.org/10.1134/S106816202305014X
- E.K.A. Abdelall, H.A.H. Elshemy, N. Ryad and A.A. Abdelaziz, Chem. Biodivers., 22, e01173 (2025); https://doi.org/10.1002/cbdv.202501173
- M. Montana, V. Montero, O. Khoumeri and P. Vanelle, Molecules, 26, 4742 (2021); https://doi.org/10.3390/molecules26164742
- X. Tang, Q. Zhou, W. Zhan, D. Hu, R. Zhou, N. Sun, S. Chen, W. Wu and W. Xue, RSC Adv., 12, 2399 (2022); https://doi.org/10.1039/D1RA07559D
- J.A. Pereira, A.M. Pessoa, M.N.D.S. Cordeiro, R. Fernandes, C. Prudêncio, J.P. Noronha and M. Vieira, Eur. J. Med. Chem., 97, 664 (2015); https://doi.org/10.1016/j.ejmech.2014.06.058
- S.M. Bellapukonda, R. Bandela, A. Singampalli, D. Srikanth, P. Kumar, S. Nanduri and V.M. Yaddanapudi, Eur. J. Med. Chem., 289, 117472 (2025); https://doi.org/10.1016/j.ejmech.2025.117472
- A.M.S. El Newahie, Y.M. Nissan, N.S.M. Ismail, D.A. Abou El Ella, S.M. Khojah and K.A.M. Abouzid, Molecules, 24, 1175 (2019); https://doi.org/10.3390/molecules24061175
- M. Montana, F. Mathias, T. Terme and P. Vanelle, Eur. J. Med. Chem., 163, 136 (2019); https://doi.org/10.1016/j.ejmech.2018.11.059
- M. Kumar, G. Joshi, S. Arora, T. Singh, S. Biswas, N. Sharma, Z.R. Bhat, K. Tikoo, S. Singh and R. Kumar, Molecules, 26, 1490 (2021); https://doi.org/10.3390/molecules26051490
- M. Alswah, A.H. Bayoumi, K. Elgamal, A. Elmorsy, S. Ihmaid and H. Ahmed, Molecules, 23, 48 (2017); https://doi.org/10.3390/molecules23010048
- P.H. Li, H. Jiang, W. Zhang, Y.-L. Li, M.-C. Zhao, W. Zhou, L.-Y. Zhang, Y.-D. Tang, C.-Z. Dong, Z.-S. Huang, H.-X. Chen and Z.-Y. Du, Eur. J. Med. Chem., 145, 498 (2018); https://doi.org/10.1016/j.ejmech.2018.01.010
- M. Sathish, B. Kavitha, V.L. Nayak, Y. Tangella, A. Ajitha, S. Nekkanti, A. Alarifi, N. Shankaraiah, N. Nagesh and A. Kamal, Eur. J. Med. Chem., 144, 557 (2018); https://doi.org/10.1016/j.ejmech.2017.12.055
- M.S. Christodoulou, M. Zarate, F. Ricci, G. Damia, S. Pieraccini, F. Dapiaggi, M. Sironi, L. Lo Presti, A.N. García-Argáez, L. Dalla Via and D. Passarella, Eur. J. Med. Chem., 118, 79 (2016); https://doi.org/10.1016/j.ejmech.2016.03.090
- R. Roskoski Jr., Pharmacol. Res., 79, 34 (2014); https://doi.org/10.1016/j.phrs.2013.11.002
- J. Sebastian, R.G. Richards, M.P. Walker, J.F. Wiesen, Z. Werb, R. Derynck, Y.K. Hom, G.R. Cunha and R.P. Di Augustine, Cell Growth Differ., 9, 777 (1998).
- F. Walker, L. Abramowitz, D. Benabderrahmane, X. Duval, D. Henin, V. Descatoire, T. Lehy and T. Aparicio, Hum. Pathol., 40, 1517 (2009); https://doi.org/10.1016/j.humpath.2009.05.010
- J. McBryan, J. Howlin, S. Napoletano and F. Martin, J. Mammary Gland Biol. Neoplasia, 13, 159 (2008); https://doi.org/10.1007/s10911-008-9075-7
- J.H. Park, Y. Liu, M.A. Lemmon and R. Radhakrishnan, Biochem. J., 448, 417 (2012); https://doi.org/10.1042/BJ20121513
References
A.K. Sahoo and A. Bhattacharyya, Curr. Org. Chem., 28, 161 (2024); https://doi.org/10.2174/0113852728285439240109071659
S. Tariq, K. Somakala and M. Amir, Eur. J. Med. Chem., 143, 542 (2018); https://doi.org/10.1016/j.ejmech.2017.11.064
T. Fonseca, B. Gigante, M.M. Marques, T.L. Gilchrist and E. De Clercq, Bioorg. Med. Chem. Lett., 12, 103 (2004); https://doi.org/10.1016/j.bmc.2003.10.013
H. Khatoon, Y. Rukayadi, S.M. Faudzi and Y. Rukayadi, ChemistrySelect, 9, e202305073 (2024); https://doi.org/10.1002/slct.202305073
A. Elfadil, A.M. Alzahrani, H. Abdullah, H. Alsamhan, T.S. Abujamel, H.E. Ahmed and A. Jiman-Fatani, Infect. Drug Resist., 16, 2291 (2023); https://doi.org/10.2147/IDR.S401371
K. Srinivas, P.V. Kumar, H. Joshi, A. Velidandi and R. Manchal, Russ. J. Bioorg. Chem., 49, 1068 (2023); https://doi.org/10.1134/S106816202305014X
E.K.A. Abdelall, H.A.H. Elshemy, N. Ryad and A.A. Abdelaziz, Chem. Biodivers., 22, e01173 (2025); https://doi.org/10.1002/cbdv.202501173
M. Montana, V. Montero, O. Khoumeri and P. Vanelle, Molecules, 26, 4742 (2021); https://doi.org/10.3390/molecules26164742
X. Tang, Q. Zhou, W. Zhan, D. Hu, R. Zhou, N. Sun, S. Chen, W. Wu and W. Xue, RSC Adv., 12, 2399 (2022); https://doi.org/10.1039/D1RA07559D
J.A. Pereira, A.M. Pessoa, M.N.D.S. Cordeiro, R. Fernandes, C. Prudêncio, J.P. Noronha and M. Vieira, Eur. J. Med. Chem., 97, 664 (2015); https://doi.org/10.1016/j.ejmech.2014.06.058
S.M. Bellapukonda, R. Bandela, A. Singampalli, D. Srikanth, P. Kumar, S. Nanduri and V.M. Yaddanapudi, Eur. J. Med. Chem., 289, 117472 (2025); https://doi.org/10.1016/j.ejmech.2025.117472
A.M.S. El Newahie, Y.M. Nissan, N.S.M. Ismail, D.A. Abou El Ella, S.M. Khojah and K.A.M. Abouzid, Molecules, 24, 1175 (2019); https://doi.org/10.3390/molecules24061175
M. Montana, F. Mathias, T. Terme and P. Vanelle, Eur. J. Med. Chem., 163, 136 (2019); https://doi.org/10.1016/j.ejmech.2018.11.059
M. Kumar, G. Joshi, S. Arora, T. Singh, S. Biswas, N. Sharma, Z.R. Bhat, K. Tikoo, S. Singh and R. Kumar, Molecules, 26, 1490 (2021); https://doi.org/10.3390/molecules26051490
M. Alswah, A.H. Bayoumi, K. Elgamal, A. Elmorsy, S. Ihmaid and H. Ahmed, Molecules, 23, 48 (2017); https://doi.org/10.3390/molecules23010048
P.H. Li, H. Jiang, W. Zhang, Y.-L. Li, M.-C. Zhao, W. Zhou, L.-Y. Zhang, Y.-D. Tang, C.-Z. Dong, Z.-S. Huang, H.-X. Chen and Z.-Y. Du, Eur. J. Med. Chem., 145, 498 (2018); https://doi.org/10.1016/j.ejmech.2018.01.010
M. Sathish, B. Kavitha, V.L. Nayak, Y. Tangella, A. Ajitha, S. Nekkanti, A. Alarifi, N. Shankaraiah, N. Nagesh and A. Kamal, Eur. J. Med. Chem., 144, 557 (2018); https://doi.org/10.1016/j.ejmech.2017.12.055
M.S. Christodoulou, M. Zarate, F. Ricci, G. Damia, S. Pieraccini, F. Dapiaggi, M. Sironi, L. Lo Presti, A.N. García-Argáez, L. Dalla Via and D. Passarella, Eur. J. Med. Chem., 118, 79 (2016); https://doi.org/10.1016/j.ejmech.2016.03.090
R. Roskoski Jr., Pharmacol. Res., 79, 34 (2014); https://doi.org/10.1016/j.phrs.2013.11.002
J. Sebastian, R.G. Richards, M.P. Walker, J.F. Wiesen, Z. Werb, R. Derynck, Y.K. Hom, G.R. Cunha and R.P. Di Augustine, Cell Growth Differ., 9, 777 (1998).
F. Walker, L. Abramowitz, D. Benabderrahmane, X. Duval, D. Henin, V. Descatoire, T. Lehy and T. Aparicio, Hum. Pathol., 40, 1517 (2009); https://doi.org/10.1016/j.humpath.2009.05.010
J. McBryan, J. Howlin, S. Napoletano and F. Martin, J. Mammary Gland Biol. Neoplasia, 13, 159 (2008); https://doi.org/10.1007/s10911-008-9075-7
J.H. Park, Y. Liu, M.A. Lemmon and R. Radhakrishnan, Biochem. J., 448, 417 (2012); https://doi.org/10.1042/BJ20121513