Fluorinated benzo-fused 1,3-diazoles, 1,2,3-triazoles, 1,2,5-thia/selenadiazoles and 1,4-diazines were synthesized and tried for cytotoxicity towards the Hep2 (laryngeal epidermoid carcinoma) cells. The diazoles, triazoles and selenadiazoles were cytotoxic with IC50 = 2.2–26.4 µM and induced the cells apoptosis at concentrations C = 1–25 µM. At the same time, they were nontoxic towards normal cells. Due to this, these scaffolds were used in the computer-aided molecular design of new antitumor agents. Particularly, novel 1,2,3-triazole and 1,3-diazole derivatives for the binding site of the PAS domain of the transcription factor HIF were designed and some of them synthesized for further study. Overall, new anticancer agents featuring apoptotic activity are suggested.
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28 September 2017
PHYSICS OF CANCER: INTERDISCIPLINARY PROBLEMS AND CLINICAL APPLICATIONS: Proceedings of the International Conference on Physics of Cancer: Interdisciplinary Problems and Clinical Applications (PC IPCA’17)
23–26 May 2017
Tomsk, Russia
Research Article|
September 28 2017
New cancer cells apoptosis agents: Fluorinated aza-heterocycles
D. O. Prima;
D. O. Prima
a)
1
Institute of Organic Chemistry SB RAS
, Novosibirsk, 630090 Russia
2
Tomsk State University
, Tomsk, 634050 Russia
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D. S. Baev;
D. S. Baev
1
Institute of Organic Chemistry SB RAS
, Novosibirsk, 630090 Russia
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E. V. Vorontsova;
E. V. Vorontsova
3
Institute of Molecular Biology and Biophysics SB RAS
, Novosibirsk, 630117 Russia
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T. S. Frolova;
T. S. Frolova
1
Institute of Organic Chemistry SB RAS
, Novosibirsk, 630090 Russia
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I. Yu. Bagryanskaya;
I. Yu. Bagryanskaya
1
Institute of Organic Chemistry SB RAS
, Novosibirsk, 630090 Russia
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Yu. G. Slizhov;
Yu. G. Slizhov
2
Tomsk State University
, Tomsk, 634050 Russia
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T. G. Tolstikova;
T. G. Tolstikova
1
Institute of Organic Chemistry SB RAS
, Novosibirsk, 630090 Russia
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A. Yu. Makarov;
A. Yu. Makarov
1
Institute of Organic Chemistry SB RAS
, Novosibirsk, 630090 Russia
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A. V. Zibarev
A. V. Zibarev
1
Institute of Organic Chemistry SB RAS
, Novosibirsk, 630090 Russia
2
Tomsk State University
, Tomsk, 634050 Russia
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a)
Corresponding author: prima.darya@gmail.com
AIP Conf. Proc. 1882, 020057 (2017)
Citation
D. O. Prima, D. S. Baev, E. V. Vorontsova, T. S. Frolova, I. Yu. Bagryanskaya, Yu. G. Slizhov, T. G. Tolstikova, A. Yu. Makarov, A. V. Zibarev; New cancer cells apoptosis agents: Fluorinated aza-heterocycles. AIP Conf. Proc. 28 September 2017; 1882 (1): 020057. https://doi.org/10.1063/1.5001636
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