| Title | SCEs and PRIs as indicators of structure-bioloical activity relationship of newly synthesized steroidal esters | |
| Author | D. Mourelatos1, Z. lakovidou1, E. Mioglou1, E. Karapidaki1, A. Koutsourea2, E. Arsenou2, M. Fousteris2 and S. Nikolaropoulos2
1Laboratory of Biology and Genetics, Medical School, Aristotle University, 54124 Thessaloniki, Greece; 2Laboratory of Pharmaceutical Chemistry, School of Health Sciences, Department of Pharmacy, University of Patras, 26504 Rion, Patra, Greece |
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| Citation | Mourelatos, D., Iakovidou, Z., Mioglou, E., Karapidaki, E., Koutsourea, A., et al.: SCEs and PRIs as indicators of structure-bioloical activity relationship of newly synthesized steroidal esters, Epitheorese Klin. Farmakol. Farmakokinet. 18(1): 52-54 (2004) | |
| Publication Date | Accepted for publication: 2004 | |
| Full Text Language | English | |
| Order – Buy | Ηλεκτρονική Μορφή: pdf (10 €) – Digital Type: pdf (10 €) pharmakonpress[at]pharmakonpress[.]gr | |
| Keywords | SCEs, PRIs, Synthesized Steroidal Esters, Structure-Biological Activity | |
| Other Terms | review article | |
| Summary | The concepts of synthesis and investigation of these compounds are the already known increased antineoplastic activity and decreased cytotoxicity of modified steroidal esters of nitrogen mustard and the knowledge that the presence of NHCO- group in modified steroidal derivatives of nitrogen mustards is important in order to lower systemic toxicity and improve specificity in cancer research. The new substances (1-6) have B-ring enlarged towards a lactam ring, additionally the products (4-6) contain the -NHCO- group inside the D5 ring and the products (1-3) have the -NHCO- group placed outside the D5 ring of steroidal nucleus and the alkylating agent has been connected by an esteric bond in the 3f2-position of the steroidal skeleton. These were compared on a molar basis, regarding their ability to induce Sister Chromatid Exchanges (SCEs) and modify Proliferation Rate Indices (PRIs) in cultured human lymphocytes. SCEs have been used as a sensitive indicator of cytogenetic damage and PRIs have been employed in order to evaluate cytostatic activity. The compounds induced statistically significant enhancement of SCEs and of cell division delays. However, the compounds 2>3>1 show increased genotoxicity and cytostatic activity compared to the others (5> 6 > 4). It seems that the introduction of the -NHCOCH3 group in the 17-0 position (exocyclically) affects the biological activity. | |
| References | 1. Camoutsis C., Trafalis D.T.P.: An overview on the antileukemic potential of D-homo-aza- and respective 17B- acetamido-steroidal alkylating esters. Intern New Drugs 21: 47-54 (2003)
2. Karayianni V., Mioglou E„ lakovidou Z., Mourelatos D., Fousteris M., Koustourea A., Arsenou E., Nikolaropoulos S.: A new approach for evaluating in vivo anti-leukemic activity using the SCE assay, An application on three newly synthesised antitumour steroidal esters. Mutation Res. 535: 79-86 (2003) 3. Ma D., Wamg G., Wang S., Kozikowski A.P., Lewin N.E., Blumberg P.M.: Synthesis and protein kinase C binding activity of benzolactam-V-7. Bioorg. Med. Chem, Lett. 5:1371-1374 (1999) 4. Endo Y., shimazu M., Fukusawa H., Driedger P.E., Ki- mura K., Tomioka N., Itai A., Shudo K.: Synthesis computer modeling and biological evaluation of novel protein kinase C agonists based on a 7- membered lactam moiety. Bioorg. Med. Chem. Lett, ft 173-178 (1999) 5. K. Goto, Maeda S., Kano Y., Sugiyama T.: Factors involved in differential Giemsa-staining of sister chromatids. Chromosoma 66: 351-359 (1978) 6. Mourelatos D.: Chromosomes study as predictor of chemoresponse of tumors. Cancer J. 9(3): 136-141 (1996) |
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Online ISSN 1011-6575
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Articles published in this Journal are Indexed or Abstracted in: • Chemical Abstracts • Elsevier’s Bibliographic Databases: Scopus, EMBASE, EMBiology, Elsevier BIOBASE SCImago Journal and Country Rank Factor
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| ΕΤΗΣΙΑ ΣΥΝΔΡΟΜΗ 2004 – ANNUAL SUBSCRIPTION 2004 | |
| Γλώσσα Πλήρους Κειμένου – Full Text Language | Αγγλικά – English |
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