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Synthesis of Novel Tetrahydrobenzazepine Derivatives and Their Cytoprotective Effect on Human Lymphocytes

Authorized Users Only
2015
Authors
Simić, Milena
Stanković, Miroslava
Mandić, Boris M.
Tešević, Vele
Savić, Vladimir
Article (Published version)
Metadata
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Abstract
Cytoprotective compounds such as amifostine play an important role in chemo-and radiotherapy due to their ability to reduce the side effects of these treatments. Our work was initiated with the intention to design, synthesise and test a new class of heterocyclic compounds that would have an antioxidative profile with the potential to be further developed as cytoprotective agents. The design was based on the privileged tetrahydrobenzazepine scaffold found in many natural products with a wide range of biological properties. This structure was further functionalised with moieties known to possess antioxidative features such as tertiary amine and styrene double bond. A series of eight tetrahydrobenzazepine derivatives of isoquinoline, 3,4-dihydro-beta-carboline and pyridine were synthesised employing the Heck reaction as a key transformation. Some of the prepared compounds were tested for their in vitro effects on chromosome aberrations in peripheral human lymphocytes using the cytochalasi...n-B blocked micronucleus (MN) assay. Three tetrahydrobenzoazepine derivatives showed significant cytoprotective properties, comparable or even better to those of the radioprotective agent amifostine.

Keywords:
Cytoprotection / Heterocycles / Micronuclei / Synthesis / Tetrahydrobenzazepine
Source:
Archiv der Pharmazie, 2015, 348, 2, 100-112
Publisher:
  • Wiley-VCH Verlag GMBH, Weinheim
Funding / projects:
  • Computational design, synthesis and biological evaluation of new heterocyclic compounds as selective tumorogenesis inhibitors (RS-172009)

DOI: 10.1002/ardp.201400350

ISSN: 0365-6233

PubMed: 25664628

WoS: 000349628500003

Scopus: 2-s2.0-84922572924
[ Google Scholar ]
2
2
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/2450
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Simić, Milena
AU  - Stanković, Miroslava
AU  - Mandić, Boris M.
AU  - Tešević, Vele
AU  - Savić, Vladimir
PY  - 2015
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2450
AB  - Cytoprotective compounds such as amifostine play an important role in chemo-and radiotherapy due to their ability to reduce the side effects of these treatments. Our work was initiated with the intention to design, synthesise and test a new class of heterocyclic compounds that would have an antioxidative profile with the potential to be further developed as cytoprotective agents. The design was based on the privileged tetrahydrobenzazepine scaffold found in many natural products with a wide range of biological properties. This structure was further functionalised with moieties known to possess antioxidative features such as tertiary amine and styrene double bond. A series of eight tetrahydrobenzazepine derivatives of isoquinoline, 3,4-dihydro-beta-carboline and pyridine were synthesised employing the Heck reaction as a key transformation. Some of the prepared compounds were tested for their in vitro effects on chromosome aberrations in peripheral human lymphocytes using the cytochalasin-B blocked micronucleus (MN) assay. Three tetrahydrobenzoazepine derivatives showed significant cytoprotective properties, comparable or even better to those of the radioprotective agent amifostine.
PB  - Wiley-VCH Verlag GMBH, Weinheim
T2  - Archiv der Pharmazie
T1  - Synthesis of Novel Tetrahydrobenzazepine Derivatives and Their Cytoprotective Effect on Human Lymphocytes
VL  - 348
IS  - 2
SP  - 100
EP  - 112
DO  - 10.1002/ardp.201400350
ER  - 
@article{
author = "Simić, Milena and Stanković, Miroslava and Mandić, Boris M. and Tešević, Vele and Savić, Vladimir",
year = "2015",
abstract = "Cytoprotective compounds such as amifostine play an important role in chemo-and radiotherapy due to their ability to reduce the side effects of these treatments. Our work was initiated with the intention to design, synthesise and test a new class of heterocyclic compounds that would have an antioxidative profile with the potential to be further developed as cytoprotective agents. The design was based on the privileged tetrahydrobenzazepine scaffold found in many natural products with a wide range of biological properties. This structure was further functionalised with moieties known to possess antioxidative features such as tertiary amine and styrene double bond. A series of eight tetrahydrobenzazepine derivatives of isoquinoline, 3,4-dihydro-beta-carboline and pyridine were synthesised employing the Heck reaction as a key transformation. Some of the prepared compounds were tested for their in vitro effects on chromosome aberrations in peripheral human lymphocytes using the cytochalasin-B blocked micronucleus (MN) assay. Three tetrahydrobenzoazepine derivatives showed significant cytoprotective properties, comparable or even better to those of the radioprotective agent amifostine.",
publisher = "Wiley-VCH Verlag GMBH, Weinheim",
journal = "Archiv der Pharmazie",
title = "Synthesis of Novel Tetrahydrobenzazepine Derivatives and Their Cytoprotective Effect on Human Lymphocytes",
volume = "348",
number = "2",
pages = "100-112",
doi = "10.1002/ardp.201400350"
}
Simić, M., Stanković, M., Mandić, B. M., Tešević, V.,& Savić, V.. (2015). Synthesis of Novel Tetrahydrobenzazepine Derivatives and Their Cytoprotective Effect on Human Lymphocytes. in Archiv der Pharmazie
Wiley-VCH Verlag GMBH, Weinheim., 348(2), 100-112.
https://doi.org/10.1002/ardp.201400350
Simić M, Stanković M, Mandić BM, Tešević V, Savić V. Synthesis of Novel Tetrahydrobenzazepine Derivatives and Their Cytoprotective Effect on Human Lymphocytes. in Archiv der Pharmazie. 2015;348(2):100-112.
doi:10.1002/ardp.201400350 .
Simić, Milena, Stanković, Miroslava, Mandić, Boris M., Tešević, Vele, Savić, Vladimir, "Synthesis of Novel Tetrahydrobenzazepine Derivatives and Their Cytoprotective Effect on Human Lymphocytes" in Archiv der Pharmazie, 348, no. 2 (2015):100-112,
https://doi.org/10.1002/ardp.201400350 . .

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