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PubMed1986

Reactions of nitrogen mustards with DNA.

This paper summarizes the mechanism of action and the covalent modifications of nucleic acids, nucleotides and nucleosides by nitrogen mustards. Nitrogen mustards react preferentially with guanine N7 in DNA in vitro. A few minor adducts have been characterized. Cross-links of nitrogen mustard and metabolites of cyclophosphamide that have been identified are diguanyl derivatives linked at N7. It is essential that studies of alkylation products in vivo be carried out, since characterization of alkylation products of cytostatic drugs should provide further insight into the mechanisms of cytotoxicity and, consequently, facilitate the development of more efficient anticancer agents. Furthermore, the monitoring of DNA adducts of therapeutic significance in patients may provide new avenues for the individualization of cancer therapy.

Acrolein↗
PubMed1985

Increased glutathione-S-transferase activity in a cell line with acquired resistance to nitrogen mustards.

A Walker 256 rat mammary carcinoma cell line (WR) resistant to bifunctional nitrogen mustards has been shown to have an approximate twofold increase in bulk glutathione-S-transferase activity compared to the parent cell line. Substrate specificity studies suggest that higher levels of Yb subunit contribute to the increased activity. By exposing WR cells to additional chlorambucil, either as a single concentration (50 micrograms/ml) or at 5 micrograms/ml for 10 days, transferase activity was further increased by up to three times the normal WR level. By using colony-forming assays, mitotic index depression, or trypan blue exclusion, the increased transferase activity could be correlated with an increase in resistance of these cells to either subsequent chlorambucil or a different bifunctional nitrogen mustard, phosphoramide mustard.

Animals↗
PubMedDate not supplied

Synthesis and evaluation of substituted naphthalimide nitrogen mustards as rationally designed anticancer compounds.

Bromonapmustine 4a and chloronapmustine 4b, two new nitrogen mustards of substituted naphthalimides, have been synthesized as mixed-function anticancer compounds from 4-bromo- and 4-chloro-N-(2-hydroxyethyl)-naphthalimide respectively following a three-step process. Their chemical alkylating activity exceeded that of nor-HN2. Their antitumour efficacy were assessed in vivo in two murine ascites tumours, namely Ehrlich ascites carcinoma (EAC) and Sarcoma-180 (S-180) by measuring the increase in median survival times (MST) of drug treated (T) over untreated control (C) mice. Two standard clinical drugs, namely endoxan (cyclophosphamide) and 5-fluorouracil (5-FU) were used as positive controls for comparison. Both of them have displayed substantial and reproducible antitumoural activity in these tumours comparable with 5-FU. These compounds inhibit the synthesis of DNA and RNA in S-180 tumour cells. These were further screened in vitro in 3 different human tumour cell lines but no significant activity was observed in those lines.

Antineoplastic Agents↗