当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > 5,10b-Ethanophenanthridine amaryllidaceae alkaloids inspire the discovery of novel bicyclic ring systems with activity against drug resistant cancer cells.

5,10b-Ethanophenanthridine amaryllidaceae alkaloids inspire the discovery of novel bicyclic ring systems with activity against drug resistant cancer cells.

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Henry S,Kidner R,Reisenauer MR,Magedov IV,Kiss R,Mathieu V,Lefranc F,Dasari R,Evidente A,Yu X,Ma X,Pertsemlidis A,Cencic R,Pelletier J,Cavazos DA,Brenner AJ,Aksenov AV,Rogelj S,Kornienko A,Frolova LV

doi

10.1016/j.ejmech.2016.05.004

subject

Has Abstract

pub_date

2016-09-14 00:00:00

pages

313-28

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30370-1

journal_volume

120

pub_type

杂志文章

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