Synthesis and biological evaluation of new C-12(α/β)-(N-) sulfamoyl-phenylamino-14-deoxy-andrographolide derivatives as potent anti-cancer agents
| Autor: | Srinivas Nanduri, Sai Giridhar Sarma Kandanur, Nageswara Rao Golakoti |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Stereochemistry
Andrographolide Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents 01 natural sciences Biochemistry Structure-Activity Relationship chemistry.chemical_compound Cell Line Tumor Drug Discovery medicine Humans Cytotoxicity Molecular Biology Cell Proliferation chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure biology 010405 organic chemistry Aryl Organic Chemistry Cancer biology.organism_classification medicine.disease Carbon 0104 chemical sciences Sulfonamide Andrographolide derivatives 010404 medicinal & biomolecular chemistry chemistry Cell culture Molecular Medicine Diterpenes Drug Screening Assays Antitumor Andrographis paniculata |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 27:2854-2862 |
| ISSN: | 0960-894X |
| Popis: | Andrographolide, the major diterpenoidal constituent of Andrographis paniculata (Acanthaceae) and its derivatives have been reported to possess plethora of biological properties including potent anti-cancer activity. In this work, synthesis and in-vitro anti-cancer evaluation of new C-12-substituted aryl amino 14-deoxy-andrographolide derivatives (III a-f) are reported. The substitutions include various sulfonamide moieties -SO2-NH-R1. The new derivatives (III a-e) exhibited improved cytotoxicity (GI50, TGI and LC50) compared to andrographolide (I) and the corresponding 3,14,19-O-triacetyl andrographolide (II) when evaluated against 60 NCI cell line panel. Compounds III c and III e are found to be non-toxic to normal human dermal fibroblasts (NHDF) cells compared to reference drug THZ-1. |
| Databáze: | OpenAIRE |
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