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New Cancer Cells Apoptosis Agents: Fluorinated Aza-Heterocycles Conference Abstracts

Conference PHYSICS OF CANCER: INTERDISCIPLINARY PROBLEMS AND CLINICAL APPLICATIONS
23-26 May 2017 , Tomsk
Journal AIP Conference Proceedings
ISSN: 0094-243X
Output data Year: 2017, Volume: 1882, Article number : 020057, Pages count : DOI: 10.1063/1.5001636
Authors Prima D.O. 1,2 , Baev D.S. 1 , Vorontsova E.V. 3 , Frolova T.S. 1 , Bagryanskaya I.Yu. 1 , Slizhov Yu.G. 2 , Tolstikova T.G. 1 , Makarov A.Yu. 1 , Zibarev A.V. 1,2
Affiliations
1 (Данные Web of science) Inst Organ Chem SB RAS, Novosibirsk 630090, Russia
2 (Данные Web of science) Tomsk State Univ, Tomsk 634050, Russia
3 (Данные Web of science) Inst Mol Biol & Biophys SB RAS, Novosibirsk 630117, Russia

Abstract: 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 mu M and induced the cells apoptosis at concentrations C = 1-25 mu M. 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.
Cite: Prima D.O. , Baev D.S. , Vorontsova E.V. , Frolova T.S. , Bagryanskaya I.Y. , Slizhov Y.G. , Tolstikova T.G. , Makarov A.Y. , Zibarev A.V.
New Cancer Cells Apoptosis Agents: Fluorinated Aza-Heterocycles
AIP Conference Proceedings. 2017. V.1882. 020057 . DOI: 10.1063/1.5001636 WOS Scopus РИНЦ OpenAlex
Identifiers:
Web of science: WOS:000426914800057
Scopus: 2-s2.0-85041651665
Elibrary: 42765382
OpenAlex: W2756560073
Citing:
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Web of science 4
Scopus 4
Elibrary 4
OpenAlex 3
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