ANTITUMOR ACTIVITY OF SOME NEW 1,3,8TRISUBSTITUTED PURINE-2,6-DIONES AND 1,3,6TRISUBSTITUTED THIAZOLO[2,3-f]PURINE-2,4DIONES | ||||
| Bulletin of Pharmaceutical Sciences Assiut University | ||||
| Article 16, Volume 31, Issue 2, December 2008, Page 391-399 PDF (153.71 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/bfsa.2008.64344 | ||||
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| Authors | ||||
| Alaa M. Hayallah* 1; Georgi Momekov2; Michael Famulok3 | ||||
| 1Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt | ||||
| 2Department of Pharmacology and Toxicology Faculty of Pharmacy, MU-Sofia 2 Dunav Str., 1000 Sofia, Bulgaria | ||||
| 3LIMES Institute, Program Unit Chemical Biology & Medicinal Chemistry, c/o Kekulé Institut für Organische Chemie, GerhardDomagk-Str.1, 53121 Bonn, Germany | ||||
| Abstract | ||||
| New 1,3,8-trisubstituted purine-2,6-diones and 1,3,6trisubstituted thiazolo[2,3-f]purine-2,4-diones were designed and synthesized as potential antitumor agents. The cytotoxic effects of the tested compounds were assessed against two human malignant cell lines: T-cell leukemia derived SKW-3 and breast cancer – derived MDA-MB-231 using the methyl thiazolyl tetrazolium (MTTdye) reduction assay, after 72 h exposure. The data were fitted to sigmoidal concentration response curves and the corresponding IC50 values were calculated using commercially available software (GraphPad Prizm). Compound AH-206 was the most potent cytotoxic agent among the newly synthesized compounds, with IC50 value of 17.3 M. Prominent activity was also encountered with compounds AH-201, AH-205, AH-208, AH-214 and AH-217, all having IC50 values below 100 µM. | ||||
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