Cytotoxic effects of C-glycosides in HOS and HeLa cell lines

Cytotoxic effects of C-glycosides in HOS and HeLa cell lines

Fifty-two C-glycosides were synthesized and their in-vitro antiproliferative activity against human cervical carcinoma (HeLa) and osteosarcoma (HOS) screened, showing significant activity. Fifty-two C-glycosides were synthesized and their in-vitro antiproliferative activity screened against human ce...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007-07, Vol.17 (13), p.3676-3681
Hauptverfasser: Sanhueza, Carlos A., Mayato, Carlos, Machı´n, Rubén P., Padrón, José M., Dorta, Rosa L., Vázquez, Jesús T.
Format: Artikel
Sprache:eng
Schlagworte:
2-Keto- C-glycosides
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Biological and medical sciences
Bone Neoplasms - drug therapy
C-Glycosides
C-Mannosides
Cancer
Cell Line, Tumor
Cell Proliferation
Cervical carcinoma (HeLa)
Cytotoxic
Drug Screening Assays, Antitumor
General aspects
Glycosides - chemistry
HeLa Cells
Humans
Inhibitory Concentration 50
Medical sciences
Models, Chemical
Osteosarcoma (HOS)
Osteosarcoma - drug therapy
Pharmacology. Drug treatments
Stereoisomerism
Structure-Activity Relationship
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Zusammenfassung:Fifty-two C-glycosides were synthesized and their in-vitro antiproliferative activity against human cervical carcinoma (HeLa) and osteosarcoma (HOS) screened, showing significant activity. Fifty-two C-glycosides were synthesized and their in-vitro antiproliferative activity screened against human cervical carcinoma (HeLa) and osteosarcoma (HOS) cell lines. Nine of them had growth inhibitions (GI 50 values) below 10 μM, the C-glucopyranoside 38 being the most active against HeLa (5.4 μM) and the dichlorocyclopropyl derivative 42 against HOS (1.6 μM). Some preliminary structure–activity relationships were established.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.060