| Title | Cytogenetic efficacy by modified steroidal esters of N-acetyl melphalan | |
| Authors | Eleni Dima¹,², Eleftheria Mioglou¹, Zafeiroula Iakovidou¹, Katerina Spyridonidou², Sotiris Nikolaropoulos² and Dionysios Mourelatos¹
1. Laboratory of Biology and Genetics, Medical School, Aristotle University, 54124 Thessaloniki, Greece 2. Laboratory of Medicinal Chemistry, Dept. of Pharmacy, University of Patras, Rion-Patras, Greece |
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| Citation | Dima, E., Mioglou, E., Iakovidou, Z., Spyridonidou, P., Nikolaropoulos, S. et al: Cytogenetic efficacy by modified steroidal esters of N-acetyl melphalan, Epitheorese Klin. Farmakol. Farmakokinet. 20(2): 85-87 (2006) | |
| Publication Date | Accepted for publication: 19-20 May 2006 | |
| Full Text Language | English | |
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| Keywords | Steroidal esters of N-Acetyl melphalan, cytogenetic effects. | |
| Other Terms | review article | |
| Summary | Melphalan (L-PAM) has been used widely in cancer chemotherapy but in many cases a diversity of toxic side effects have been reported. The chemical linkage with a steroidal moiety has been proven one of the most effective strategies in order to reduce the high toxicity and ameliorate the selectivity of alkylating agents. Six newly synthesized N-Ac-Melphalan esters with modified steroidal skeletons at D and/or B ring have been tested, on a molar basis (0.1 and 0.2 µM) for cytogenetic activity in normal human lymphocyte cultures. SCEs have been used as the most sensitive indicator of DNA damage and/or subsequent repair and PR/ as a very valuable index of cytostatic effects. All derivatives induced a dose dependent significant increase (P<0.001) in SCE frequency and the most effective proved the 7-17-diketo compound. A correlation was observed between the magnitude of SCE response and the PR/ depression (r = -0.55, and P<0.02). Ιt is of interest that N-Ac-Melphalan and Melphalan at 0.1 µM were inactive, while the six steroidal derivatives proved quite effective. | |
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Online ISSN 1011-6575
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