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Nitric oxide-donating derivatives of hederacolchiside A 1 : Synthesis and biological evaluation in vitro and in vivo as potential anticancer agents.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Jan 01; Vol. 27 (1), pp. 98-101. Date of Electronic Publication: 2016 Nov 10. - Publication Year :
- 2017
-
Abstract
- A series of nitric oxide (NO) donating derivatives of hederacolchiside A <subscript>1</subscript> bearing triterpenoid saponin motif were designed, synthesized and evaluated for their anticancer activity. All of the tested furoxan-based NO releasing compounds showed significant proliferation inhibitory activities. Especially compound 6a exhibited strong cytotoxicity (IC <subscript>50</subscript> =1.6-6.5μM) against four human tumor cell lines (SMMC-7721, NCI-H460, U251, HCT-116) in vitro and the highest level of NO releasing. Furthermore, compound 6a was revealed low acute toxicity to mice and weak haemolytic activity with potent tumor growth inhibition against mice H22 hepatocellular cells in vivo (51.5%).<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Mice
Molecular Structure
Neoplasms, Experimental drug therapy
Neoplasms, Experimental pathology
Nitric Oxide chemistry
Saponins chemical synthesis
Saponins chemistry
Structure-Activity Relationship
Antineoplastic Agents pharmacology
Nitric Oxide pharmacology
Saponins pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 27
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 27866816
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.11.021