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5,10b-Ethanophenanthridine amaryllidaceae alkaloids inspire the discovery of novel bicyclic ring systems with activity against drug resistant cancer cells
- Source :
- European journal of medicinal chemistry, 120
- Publication Year :
- 2016
-
Abstract
- Plants of the Amaryllidaceae family produce a large variety of alkaloids and non-basic secondary metabolites, many of which are investigated for their promising anticancer activities. Of these, crinine-type alkaloids based on the 5,10b-ethanophenanthridine ring system were recently shown to be effective at inhibiting proliferation of cancer cells resistant to various pro-apoptotic stimuli and representing tumors with dismal prognoses refractory to current chemotherapy, such as glioma, melanoma, non-small-cell lung, esophageal, head and neck cancers, among others. Using this discovery as a starting point and taking advantage of a concise biomimetic route to the crinine skeleton, a collection of crinine analogues were synthetically prepared and evaluated against cancer cells. The compounds exhibited single-digit micromolar activities and retained this activity in a variety of drug-resistant cancer cell cultures. This investigation resulted in the discovery of new bicyclic ring systems with significant potential in the development of effective clinical cancer drugs capable of overcoming cancer chemotherapy resistance.<br />SCOPUS: ar.j<br />info:eu-repo/semantics/published
- Subjects :
- 0301 basic medicine
Haemanthamine
Amaryllidaceae Alkaloid
medicine.medical_treatment
Antineoplastic Agents
Drug resistance
Pharmacology
Pharmacologie
Multidrug resistance
Lycorine
Article
Plant Extract
Antineoplastic Agent
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Drug Discovery
medicine
Tumor Cells, Cultured
Humans
Amaryllidaceae Alkaloids
Chemotherapy
Translation inhibition
Bicyclic molecule
Chemistry
Plant Extracts
Melanoma
Organic Chemistry
Amaryllidaceae
General Medicine
medicine.disease
3. Good health
Multiple drug resistance
Chimie organique
030104 developmental biology
Drug Resistance, Neoplasm
030220 oncology & carcinogenesis
Cancer cell
Apoptosis resistance
Glioblastoma
Human
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- European journal of medicinal chemistry, 120
- Accession number :
- edsair.doi.dedup.....7b3e3ad72a05755f6291272e48937e29