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

• Published in: Bioorganic & medicinal chemistry letters Vol. 17; no. 13; pp. 3676 - 3681
• Main Authors: Sanhueza, Carlos A., Mayato, Carlos, Machı´n, Rubén P., Padrón, José M., Dorta, Rosa L., Vázquez, Jesús T.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.07.2007; Elsevier
• Subjects: 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; C-Glycosides; 2-Keto- C-glycosides; Osteosarcoma (HOS); Cervical carcinoma (HeLa); Cytotoxic; C-Mannosides; Cancer; Antineoplastic agent; Human; Cytotoxicity; Uterine cervix; Oxygen heterocycle; Organic chlorine compounds; In vitro; Hela cell line; Cell line; Structure activity relation; Bicyclic compound; Bone; C-Glycoside; Chemical synthesis; 2-Keto-C-glycosides; Tumor cell
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2007.04.060

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.