New Cancer Cells Apoptosis Agents: Fluorinated Aza-Heterocycles

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

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.

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

Web of science	WOS:000426914800057
Scopus	2-s2.0-85041651665
Elibrary	42765382
OpenAlex	W2756560073