Τόμος 2 (1988) – Τεύχος 1 – Άρθρο 4 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 2 (1988) – Issue 1 – Article 4 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

Title Structure-antileukemic activity relationships of modified steroidal alkylating agents in P388 and L1210 murine leukemias
Author Panayotis Catsoulacos

Laboratory of Pharmaceutical Chemistry, University of Patras, Greece

Citation Catsoulacos, P.: Structure-antileukemic activity relationships of modified steroidal alkylating agents in P388 and L1210 murine leukemias, Epitheorese Klin. Farmakol. Farmakokinet. 2(1): 45-50 (1988)
Publication Date 1988-07
Full Text Language English
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Keywords Leukemia, aza-steroidal esters, L1210, P388, steroidal alkylating agent, effects.
Other Terms review article
Summary In this review article we report the activity of aza-steroidal esters in early and advanced L1210 and P388 murine leukemias. Our activity relationship studies of steroidal alkylating agent suggest that, in addition to an easily cleaved ester bond, which is basic requirement for antitumor activity, the lactam moiety is required for activity in P388 and L1210 leukemias.
References 1. Niculescu-Ouvaz, I. and Baracu, D.: Selection of carriers for alkylating moities to increase their antitumor specificity: A different aspect. Cancer Treat. Rep. 61: 929 (1977)

2.         Wall, M.E., Abernethy, G.S., Carroll, F.l. and Taylor, D.J.: The effects of some steroidal alkylating agent on experimental animal mammary tumor and leukemia systems. Λ Med. Chem. 12: 810 (1969)

3.         Hogberg, K.B., Fex, H.J., Konyves, I. and Kneip, H.O.J.: Steroid esters. German Patent 1: 249, 862 (1967)

4.         Fex, H.J., Hogberg, K.B. and Konyves, I.: Corticosteroid p-bis(2-chtoroethyl) aminophenylcarboxylates as antitumor agents. Ger. Of fen 2. 001, 305, 1970: Chem. Abstr. 73.        99119 (1970)

5.         Catsoulacos, P. and Boutis, L.: Aza-steroids. Beckman re-arrangement of 3{3-acetoxy-5o-androstan-17-one oxime acetate with boron fluoride. Alkylating agents. £ur. J. Med Chem. 8: 215 (1973)

6.         Wampler, G.L and Catsoulacos, P.: Antileukemic effect of homo-aza-steroidal-ester of [p-bis(2-chloroethyl}amino] phenylacetic acid. Cancer Treat. Rep. 61: 37 (1977)

7.         Catsoulacos, P. and Politis, D.: Antileukemic effects of the homo-aza-steroidal ester of [p-bis(2-chloroethyl)amino] phenylthioacetic acid. Eur. J. Med. Chem. 14: 95 (1979)

8.         Catsoulacos, P., Politis, D. and Wampler, G.L.: Antitumor activity of [p-bis(2-chloroethyl)amino]phenylbutyric acid. Cancer Chemother. Pharmacol. 10: 129 (1983)

9.         Catsoulacos, P., Politis, D., Boutis, L. and Papageorgiou, A.: Antitumor activity of 3p-hydroxy-13a-amino-13,17-seco- 5a-androstan-17-oic-13,17-lactam-4-N,N,-bis(2-chloro- ethyl)amino phenylbutyrate. J. Pharm. Sci. 67: 1342 (1978)

10.       Catsoulacos, P., Politis, D. and Wampler. G.L.: A new steroidal alkylating agent with improved activity in advanced murine leukemia. Cancer Chemother. Pharmacol. 3: 67 (1979)

11.       Catsoulacos, P. and Politis, D.: Synthesis of steroidal N,N- bis(2-chloroethyl)carbamates and their effects in murine leukemias. Eur. J. Med. Chem. 16: 181 (1981)

12.       Catsoulacos, P., Camoutsis, Ch. and Wampler, G.L.: Effect of homo-aza-steroidal ester in P388 and L1210 murine leukemia. Oncology, 39: 59 (1982)

13.       Catsoulacos, P. and Boutis, L.: Antitumor activity of a homo-aza-steroidal ester of [p-bis(2-chloroethyl)amino] phenylacetic acid. Cancer Chemother. Rep. 57:365 (1973)

14.       Catsoulacos, P. and Boutis, L.: Cytostatic action of 3β- hydroxy-13a-amino-13,17-seco-5-androsten-17-oic-13, 17-lactam-p-N,N-bis(2-chloroethyl)aminopheny(acetate. Eur. J. Med. Chem. 9: 211 (1974)

15.       Politis, G., Camoutsis, Ch. and Catsoulacos, P: Proliferation of human acute leukemia cells in culture on treatment with an homo-aza-steroid. Methods and Findings 4: 403 (1982)

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