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Article . 2011
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Bioorganic & Medicinal Chemistry Letters
Article . 2011 . Peer-reviewed
License: Elsevier TDM
Data sources: Crossref
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Design, synthesis and antiproliferative activity of novel aminosubstituted benzothiopyranoisoindoles

Authors: Christodoulou, A.; Kostakis, I.K.; Kourafalos, V.; Pouli, N.; Marakos, P.; Trougakos, I.P.; Tsitsilonis, O.E.;

Design, synthesis and antiproliferative activity of novel aminosubstituted benzothiopyranoisoindoles

Abstract

The synthesis of a number of new benzothiopyrano[4,3,2-cd]isoindole aminoderivatives designed as structural analogues of the key metabolite of the anticancer agent Ledacrine (nitracrine) and their in vitro cytotoxic activity evaluation against HCT-116, MES-SA, and MES-SA/Dx cancer cell lines is reported. The majority of the derivatives possessed noticeable cytotoxicity in a low μM range indicating an interesting structure-activity relationship.

Country
Greece
Keywords

Indoles, Molecular Structure, Antineoplastic Agents, Inhibitory Concentration 50, Structure-Activity Relationship, Cell Line, Tumor, Drug Design, Humans, Nitracrine, Sulfhydryl Compounds, Amines, Cell Proliferation, Pyrans

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    This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    9
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Average
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
9
Average
Average
Top 10%
Green