title: Anticancer activity of dinuclear gallium(III) carboxylate complexes.
abstract: The reaction of 3-methoxyphenylacetic acid, 4-methoxyphenylacetic acid, mesitylthioacetic acid, 2,5-dimethyl-3-furoic acid and 1,4-benzodioxane-6-carboxylic acid with trimethylgallium (1:1) yielded the dimeric complexes [Me(2)Ga(micro-O(2)CCH(2)C(6)H(4)-3-OMe)](2) (1), [Me(2)Ga(micro-O(2)CCH(2)C(6)H(4)-4-OMe)](2) (2), [Me(2)Ga(micro-O(2)CCH(2)SMes)](2) (3) (Mes=2,4,6-Me(3)C(6)H(2)), [Me(2)Ga{micro-O(2)C(Fur)}](2) (4) (Fur=2,5-dimethylfuran) and [Me(2)Ga{micro-O(2)C(Bdo)}](2) (5) (Bdo=1,4-benzodioxane) respectively. The molecular structure of 5 was determined by X-ray diffraction studies. The cytotoxic activity of the gallium(III) complexes (1-5) was tested against human tumor cell lines 8505C anaplastic thyroid cancer, A253 head and neck tumor, A549 lung carcinoma, A2780 ovarian cancer, DLD-1 colon carcinoma and compared with that of cisplatin. Taking into account the standard deviation, there is no significant difference in the activity for any of the compounds in any cell line. However, complex 5 presents the best IC(50) value against A253 head and neck tumor (6.6+/-0.2 microM), while complex 3 seems to be the most active against A2780 ovarian cancer (12.0+/-0.4 microM) and marginally on DLD-1 colon carcinoma (12.4+/-0.1 microM).
authors.affiliation: Department of Oral, Maxillofacial and Facial Plastic Surgery, University of Leipzig, Nürnberger Str 57, D-04103 Leipzig, Germany.
authors.forename: Milena R
authors.initials: MR
authors.lastname: Kaluderović
authors.forename: Santiago
authors.initials: S
authors.lastname: Gómez-Ruiz
authors.forename: Beatriz
authors.initials: B
authors.lastname: Gallego
authors.forename: Evamarie
authors.initials: E
authors.lastname: Hey-Hawkins
authors.forename: Reinhard
authors.initials: R
authors.lastname: Paschke
authors.forename: Goran N
authors.initials: GN
authors.lastname: Kaluderović
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D005708:Gallium / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D008968:Molecular Conformation; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013057:Spectrum Analysis
chemical_list: D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D009942:Organometallic Compounds; D005708:Gallium