| Title | Modified steroid molecules as biological platforms of cytotoxic groups: carboxylic derivatives of N,N-bis-2-(chloroethyl) aniline | |
| Author | Panayotis Catsoulacos
Laboratory of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, University of Patras, Patra, Greece |
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| Citation | Catsoulacos, P.: Modified steroid molecules as biological platforms of cytotoxic groups: carboxylic derivatives of N,N-bis-2-(chloroethyl) aniline, Epitheorese Klin. Farmakol. Farmakokinet. 4(1): 24-37 (1990) | |
| Publication Date | Received for publication: September, 10, 1989
Accepted for publication: October 29, 1989 |
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| Full Text Language | English | |
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| Keywords | Modified steroid molecules, antineoplatic activity. | |
| Other Terms | review article | |
| Summary | The homo-aza-steroidal esters of p-N,N-bis(2-chloroethyl)aminophenylacetic acid, p-N,N-bis(2-chloroethyl)aminophenyibutyric acid and p-N,N-bis(2-chloroethyl)aminophenoxyacetic acid are active in several experimental animal tumors. Steroidal lactone esters of p-N,N-bis(2-chloroethyl)aminophenylacetic acid showed moderate activity in tumor T8 and practically no effect on melanoma B16 and Theagenion-Bahner angiosarcoma. Since the antineoplastic activity of some of the steroidallactam-esters is superior than the older or unmodified steroidal alkylating agents and because of the activity shown against human tumor xenografts, these drugs are an attractive candidate for clinical trial. As far as we know, there is no information about the sensitivity of MX-1 and LX-1 xenograft systems against the nitrogen mustards. | |
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2. Regan, B.M., Hayes, N.: 17 and 17a-aza-D-homosteroids. J. Amer. Chem. Soc. 78: 639 (1956) 3. Levy, H., Jacobsen, R.P.: Steroid lactones. The preparation of isoandrolic acid and related compounds. J. Biol. Biochem. 171: 71 (1947) 4. Catsoulacos, P., Boutis, L.: Aza-steroids. Beckman re-arrangement of 3p-acetoxy-5a-androstan-17-one oxime acetate with boron fluoride. Alkylating agents. Eur. J. Med. Chem. 8: 215 (1973) 5. Catsoulacos, P., Boutis, L.: Antitumor activity of a homo-aza-steroidal ester of [p-bis(2-chloroethyl)amino] phenylacetic acid. Cancer Chemother. Rep. 57: 365 (1973) 6. Catsoulacos, P., Boutis, L.: Cytostatic action of 3p-hy- droxy-13a-amino-13,17-seco-5-androsten-17-oic-13,17- lactam,-p-N,N-bis(2-chloroethyl)aminophenylacetate. Eur. J. Med. Chem. 9: 211 (1974) 7. Catsoulacos, P., Politis, D., Boutis, L. et al.: Antitumor activity of 3p-hydroxy-13a-amino-13,17-seco-5a-androstan-17-oic-13,17-lactam-4-N,N-bis(2-chloroethyl)aminoi phenylbutyrate. J. Pharm. Sci. 67: 1342 (1978) 8. Catsoulacos, P., Boutis. L., Dlmitropoulos, K.: Antitumor activity of steroidal lactone esters of bis(2-chloroethyl} aminophenylacetic acid. Eur. J. Med. Chem. 11: 189 (1976) 9. Catsoulacos, P., Wampler, G.L.: Activity of 3p-hydroxy- 13a-amino-13,17-seco-5a-androstan-17-oic-13,17- lactam[p-(bis(2-chloroethyl)amino[acetate (NSC 290205) in murine solid tumors. Ongology 39: 109 (1982) 10. Catsoulacos, P.: Further studies of the antineoplastic activity of 3p-hydroxy-13a-amino-13,17-seco-5a-androstan-17-oic-13,17-lactam-p-bis(2-chloroethyl)aminophenylacetate. Cancer Let. 22: 199 (1984) 11. Catsoulacos, P.: Activity of 3p-hydroxy-13a-amino-13, 17-seco-5a-androstan-17-oic-13,17-lactam-p-bis (2-chloroethyl)aminophenoxyacetate (NSC 294859) on experimental animal tumor and leukemia systems. Ongology 40: 240 (1983) |
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Online ISSN 1011-6575
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