Τόμος 10 (1996) – Τεύχος 1 – Άρθρο 6 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 10 (1996) – Issue 1 – Article 6 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

Title New compound: activity of 17β-hydroxy-3-aza-A-homo-4α-androsten-4-one-p-N,N-bis(2-chloroethyl)-aminophenoxy-acetate in P388 and L1210 leukemias
Authors Dimitris Catsoulacos and Panayotis Catsoulacos

Laboratory of Pharmaceutical Chemistry, Department of Pharmacy, School of Health and Sciences, University of Patras, Patra, Greece

Citation Catsoulacos, D., Catsoulacos, P.: New compound: activity of 17β-hydroxy-3-aza-A-homo-4α-androsten-4-one-p-N, N-bis(2-chloroethyl)-aminophenoxy-acetate in P388 and L1210 leukemias, Epitheorese Klin. Farmakol. Farmakokinet. 10(1): 38-40 (1996)
Publication Date Received for publication: 1 February 1996

Accepted for publication: 15 February 1996

Full Text Language English
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Keywords Homo-aza-steroidal ester, antileukemic activity.
Other Terms review article
Summary The new compound 17β-hydroxy-3-aza-A-homo-4α-androsten-4-one-p-N,N-bis(2-chloroethyl)-aminophenoxy-acetate was prepared by reacting 4-[p-bis(2-chloroethyl)amino]phenoxy-acetyl chloride with 17β-hydroxy-A-homo-4α-androsten-4-one. The antileukemic activity of the ester was investigated in L1210 and P388 leukemias. The steroidal congener is inactive in P388 leukemia.
References 1.     Catsoulacos P., Boutis L.: Aza-steroids. Beckmann rearrangement of 3β-acetoxy-5α-androstan-17-one oxime acetate with boron fluoride. Alkylating agents. Chim. Ther. 8: 215-217 (1973)

2.     Wall M.E., Abernethy G.R., Carroll F.J., Taylor D.J.: The effect of some steroidal alkylating agents on experimental animal mammary tumor and leukemia systems. J. Med Chem. 12: 810-818 (1969).

3.     Wampler G.L., Catsoulacos P.: Antileukemic effect of homo-aza-steroidal ester of p-bis(2-chloroethyl)aminophenylacetic acid. Cancer Treat. Rep. 61: 37-41 (1977)

4.     Catsoulacos P., Politis D., Wampler G.L.: A new steroidal alkylating agent with improved activity in advanced murine leukemias. Cancer Chemother. Pharmacol. 3 : 67-70 (1970)

5.     Catsoulacos P., Politis D., Wampler G.L.: Antitumor activity of homo-aza-steroidal esters of p-bis(2-chloroethyl)aminophenylacetic acid and p-bis(2-chloroethyl)aminophenylbutyric acid. Cancer Chemother. Pharmacol. 10: 129-132 (1983)

6.     Catsoulacos P., Camoutsis Ch., Wampler G.L.: Effect of an homo-aza-steroidal ester in P388 and L1210 murine leukemias. Oncology 30: 59-60 (1989)

7.     Catsoulacos P., Boutis L.: Antitumor activity of an homo-aza-steroidal ester of p-bis(2-chloroethyl)aminophenylacetic acid. Cancer Chemoth. Rep. 57: 365- 367 (1973)

8.     Catsoulacos P.: Activity of 3(3-hydroxy-13α-amino-13,17-seco-5α-androstan-17-oic-13,17-lactam-p-bis(2-chloroethyl)aminophenoxyacetate in experimental animal tumor and leukemia systems. Oncology 40: 240-243 (1983)

9.     Catsoulacos P.: Further studies on the antineoplastic activity of 3p-hydroxy-13α-amino-13,17-seco-5α-andro-stan-17-oic-13,17-lactam-p-bis(2-chloroethyl)aminophenylacetate. Cancer Let. 22: 199-202 (1984)

10.  Catsoulacos P.: Beckmann rearrangement of testosterone oximes. Chimika Chronica, New Series 1: 147-150 (1972). [Mazur R.H.: J. Org. Chem. 28: 248 (1963)]

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