Synthesis of Bis(Aziridinyl) Phosphinic Amide Derivatives of Thymidine as Potential Anticancer Agents
- 1 June 1988
- journal article
- research article
- Published by Taylor & Francis in Nucleosides, Nucleotides and Nucleic Acids
- Vol. 7 (3) , 403-408
- https://doi.org/10.1080/07328318808068720
Abstract
3′- and 5′-Bis(aziridinyl)phosphinic amide derivatives of thymidine have been synthesized as potential anticancer agents from 3′-amino-3′-deoxythymidine and 5′-amino-5′-deoxythymidine, respectively. The aziridine-containing compounds were tested for their cytotoxic action in vitro against the L1210 leukemia; the 3′-bis(aziridinyl)phosphinic amide derivative was found to be about 11-times more active than its 5′-counterpart in inhibiting the replication of these leukemic cells, with ED50 values of 0.6 and 7 μM, respectively, being obtained.This publication has 15 references indexed in Scilit:
- Synthesis of 5'-thymidinyl bis(1-aziridinyl)phosphinates as antineoplastic agentsJournal of Medicinal Chemistry, 1981
- Absence of cross-resistance to alkylating agents in cyclophosphamide-resistant L1210 leukemiaPublished by Elsevier ,1978
- Synthesis and biological activity of several amino analogs of thymidineJournal of Medicinal Chemistry, 1978
- Cyclophosphamide, 2,2-dimethylaziridines and other alkylating agents as inhibitors of serum cholinesteraseBiochemical Pharmacology, 1975
- Synthesis of bis(aziridinyl)phosphinyl-N-hydroxyurethane derivatives as antineoplastic agentsJournal of Medicinal Chemistry, 1975
- Combination of chemotherapy with dual antagonists and radiotherapy in the treatment of neoplastic diseaseJournal of Surgical Oncology, 1971
- STRUCTURE-ACTIVITY RELATIONSHIPS OF ALKYLATING AGENTS IN CANCER CHEMOTHERAPYAnnals of the New York Academy of Sciences, 1969
- Studies on the chemistry, antitumor activity, and pharmacology of ethyl Di-(2,2 -dimethyl)ethylenamido phosphate (AB-163)Journal of Surgical Oncology, 1969
- Synthesis of Potential Dual Antagonists IIIJournal of Pharmaceutical Sciences, 1965
- Consideration of chemical reaction mechanisms in relationship to the biological action of “dual antagonists”Biochemical Pharmacology, 1962