PMID- 21194614 OWN - NLM STAT- MEDLINE DCOM- 20110516 LR - 20131121 IS - 1873-3344 (Electronic) IS - 0162-0134 (Linking) VI - 105 IP - 2 DP - 2011 Feb TI - Organogallium(III) complexes as apoptosis promoting anticancer agents for head and neck squamous cell carcinoma (HNSCC) cell lines. PG - 164-70 LID - 10.1016/j.jinorgbio.2010.10.013 [doi] AB - Organogallium(III) dinuclear (1-9) and tetranuclear (10) complexes present potential therapeutic agents for the treatment of various types of cancer. The antiproliferative activity of 1-10 was evaluated with cell lines of head and neck squamous cell carcinomas, e.g. HN (soft palate), Cal27, Cal33 (tongue) and FaDu (hypopharynx) cell lines. The activity of compound 8 is comparable with that of cisplatin on cell line Cal27 (IC(50) 4.6 muM for both compounds). The mode of cell death induced, caspase activity and cell cycle analysis were evaluated for potential hit compounds 3, 5 and 8 Potential hit compounds 3, 5 and 8 were further evaluated for the mode of cell death, caspase activity and cell cycle analysis. Apoptosis induced by compounds 3, 5 and 8 on Cal27 and FaDu cells was confirmed by DNA laddering , as well as acridine orange (AO) and ethidium bromide (EB) double staining. These compounds (3, 5 and 8) induced caspase-independent apoptosis (within 4 h of action) in cell line Cal27. Extrinsic-mediated apoptosis associated with caspase 8 and 3 activation is the main mode of cytotoxicity induced on FaDu cells by compounds 3, 5 and 8. Cell cycle perturbations caused by these compounds are also observed. Our data suggest that compounds 3, 5 and 8 should be studied further for the treatment of head and neck cancer. CI - Copyright A(c) 2010 Elsevier Inc. All rights reserved. FAU - Kaluderovic, Milena R AU - Kaluderovic MR AD - Department of Oral, Maxillofacial and Facial Plastic Surgery, University of Leipzig, Nurnberger Str. 57, D-04103 Leipzig, Germany. FAU - Kaluderovic, Goran N AU - Kaluderovic GN FAU - Gomez-Ruiz, Santiago AU - Gomez-Ruiz S FAU - Paschke, Reinhard AU - Paschke R FAU - Hemprich, Alexander AU - Hemprich A FAU - Kuhling, Jan AU - Kuhling J FAU - Remmerbach, Torsten W AU - Remmerbach TW LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20101030 PL - United States TA - J Inorg Biochem JT - Journal of inorganic biochemistry JID - 7905788 RN - 0 (Antineoplastic Agents) RN - 0 (Coordination Complexes) RN - CH46OC8YV4 (Gallium) RN - EC 3.4.22.- (Caspases) SB - IM MH - Antineoplastic Agents/chemistry/*pharmacology MH - Apoptosis MH - Carcinoma, Squamous Cell MH - Caspases/metabolism MH - Cell Cycle/drug effects MH - Cell Line, Tumor MH - Cell Survival/drug effects MH - Coordination Complexes/chemistry/*pharmacology MH - DNA Fragmentation/drug effects MH - Drug Screening Assays, Antitumor MH - *Gallium MH - Head and Neck Neoplasms MH - Humans MH - Inhibitory Concentration 50 MH - Structure-Activity Relationship EDAT- 2011/01/05 06:00 MHDA- 2011/05/17 06:00 CRDT- 2011/01/04 06:00 PHST- 2010/07/19 00:00 [received] PHST- 2010/10/24 00:00 [revised] PHST- 2010/10/25 00:00 [accepted] PHST- 2011/01/04 06:00 [entrez] PHST- 2011/01/05 06:00 [pubmed] PHST- 2011/05/17 06:00 [medline] AID - S0162-0134(10)00241-2 [pii] AID - 10.1016/j.jinorgbio.2010.10.013 [doi] PST - ppublish SO - J Inorg Biochem. 2011 Feb;105(2):164-70. doi: 10.1016/j.jinorgbio.2010.10.013. Epub 2010 Oct 30.