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Gilles Gallant - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and anti-HIV activity of new urea and nitrosourea derivatives of diamino acids.
Bioorganic & Medicinal Chemistry, 1995Co-Authors: Hélène Dulude, Romano Salvador, Gilles GallantAbstract:Abstract A series of N 1 -methyl, N 1 -allyl, N 1 -(2-chloroethyl) and N 1 -propargyl urea and nitrosourea derivatives of diamino acids ( l -omithine and l -lysine) was synthesized and was shown to have weak activity in counteracting the cytopathic effects of the HIV-1 on a T 4 lymphocyte cell line (CEM-IW). However, selected compounds may possess some immunomodulatory activity. A series of N 1 -methly, N 1 -allyl, N 1 (2-chloroethyl) and N 1 -propargyl urea and nitrosourea derivatives of diamino acids ( l -ornithine and l -lysine) was synthesized and was shown to have weak activity in counteracting the cytopathic effects of the HIV-1 on a T 4 lymphocyte cell line (CEM-IW). However, selected compounds may possess some immunomodulatory activity.
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Chemical stability of new urea and nitrosourea derivatives of diamino acids.
Bioorganic & Medicinal Chemistry Letters, 1994Co-Authors: Hélène Dulude, Romano Salvador, Gilles GallantAbstract:Abstract Stability in neutral aqueous solutions of a series of nitrosourea derivatives of diamino acids was determined. Structure-activity relationships show that N 3 -bisubstitution increased the stability of these compounds. Moreover, in N 3 -monosubstituted and N 3 -bisubstituted compounds, stability is : N 1 -Methyl > N 1 -Allyl > N 1 -2-Chloroethyl > N 1 -Propargyl. Stability in neutral aqueous solutions of a series of nitrosourea derivatives of diamino acids was determined. Structure-activity relationships show that N 3 -bisubstitution increased the stability of these compounds. Moreover, in N 3 -monosubstituted and N 3 -bisubstituted compounds, stability is : N 1 -Methyl > N 1 -Allyl > N 1 -2-Chloroethyl > N 1 -Propargyl.
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Synthesis, anti-HIV and anti-Proliferative Activity of New Urea and Nitrosourea Derivatives of Amino Acids
Antiviral Chemistry and Chemotherapy, 1991Co-Authors: Gilles Gallant, Romano Salvador, Hélène DuludeAbstract:A series of N-methyl, N-(2-chloroethyl) and N-propargyl urea and nitrosourea derivatives of amino acids were synthesized and tested for anti-HIV and anti-proliferative activity. All the agents tested showed only a weak activity to counteract the cytopathic effects of the HIV-1 virus on a T4 lymphocyte cell line (CEM-IW). At high concentration, the N-methyl and N-propargyl ureas were cytotoxic. The nitrosoureas failed to suppress cell proliferation of uninfected CEM-IW cells. The lack of activity and cytotoxicity of the nitrosoureas in this model could be explained by their short chemical half-life.
E. Beuls - One of the best experts on this subject based on the ideXlab platform.
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Isolation and preliminary characterization of ACNU-resistant sublines of rat brain tumors in vivo.
Journal of Neurosurgery, 1992Co-Authors: Yoshida T, Keiji Shimizu, A. Koulousakis, Virginia E. Sturm, E. BeulsAbstract:✓ Two variant cells lines resistant to the nitrosourea derivative ACNU ((1-4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea hydrochloride), namely C6/ACNU and 9L/ACNU, were selected in vivo from rat brain tumors. Stable resistance to ACNU proved to be a characteristic of these cell lines, whether they were grown in vivo or in vitro. These cell lines exhibited a different pattern of cross-resistance to a wide range of chemotherapeutic agents with dissimilar chemical structures and mechanisms of action as compared with that of other ACNU-resistant cell lines established in vitro. Distinct cross-resistance was observed in both the C6/ACNU and 9L/ACNU cell lines to chloroethyl-nitrosoureas such as BCNU (carmustine), CCNU (lomustine), and methyl CCNU and, additionally, to vincristine, vinblastine, Adriamycin (doxorubicin), and arabinosylcytosine, but not to bleomycin, methotrexate, c/s-platinum, and 5-fluorouracil. This might point to a multifactorial mechanism of drug resistance in ACNU-r...
Hélène Dulude - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and anti-HIV activity of new urea and nitrosourea derivatives of diamino acids.
Bioorganic & Medicinal Chemistry, 1995Co-Authors: Hélène Dulude, Romano Salvador, Gilles GallantAbstract:Abstract A series of N 1 -methyl, N 1 -allyl, N 1 -(2-chloroethyl) and N 1 -propargyl urea and nitrosourea derivatives of diamino acids ( l -omithine and l -lysine) was synthesized and was shown to have weak activity in counteracting the cytopathic effects of the HIV-1 on a T 4 lymphocyte cell line (CEM-IW). However, selected compounds may possess some immunomodulatory activity. A series of N 1 -methly, N 1 -allyl, N 1 (2-chloroethyl) and N 1 -propargyl urea and nitrosourea derivatives of diamino acids ( l -ornithine and l -lysine) was synthesized and was shown to have weak activity in counteracting the cytopathic effects of the HIV-1 on a T 4 lymphocyte cell line (CEM-IW). However, selected compounds may possess some immunomodulatory activity.
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Chemical stability of new urea and nitrosourea derivatives of diamino acids.
Bioorganic & Medicinal Chemistry Letters, 1994Co-Authors: Hélène Dulude, Romano Salvador, Gilles GallantAbstract:Abstract Stability in neutral aqueous solutions of a series of nitrosourea derivatives of diamino acids was determined. Structure-activity relationships show that N 3 -bisubstitution increased the stability of these compounds. Moreover, in N 3 -monosubstituted and N 3 -bisubstituted compounds, stability is : N 1 -Methyl > N 1 -Allyl > N 1 -2-Chloroethyl > N 1 -Propargyl. Stability in neutral aqueous solutions of a series of nitrosourea derivatives of diamino acids was determined. Structure-activity relationships show that N 3 -bisubstitution increased the stability of these compounds. Moreover, in N 3 -monosubstituted and N 3 -bisubstituted compounds, stability is : N 1 -Methyl > N 1 -Allyl > N 1 -2-Chloroethyl > N 1 -Propargyl.
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Synthesis, anti-HIV and anti-Proliferative Activity of New Urea and Nitrosourea Derivatives of Amino Acids
Antiviral Chemistry and Chemotherapy, 1991Co-Authors: Gilles Gallant, Romano Salvador, Hélène DuludeAbstract:A series of N-methyl, N-(2-chloroethyl) and N-propargyl urea and nitrosourea derivatives of amino acids were synthesized and tested for anti-HIV and anti-proliferative activity. All the agents tested showed only a weak activity to counteract the cytopathic effects of the HIV-1 virus on a T4 lymphocyte cell line (CEM-IW). At high concentration, the N-methyl and N-propargyl ureas were cytotoxic. The nitrosoureas failed to suppress cell proliferation of uninfected CEM-IW cells. The lack of activity and cytotoxicity of the nitrosoureas in this model could be explained by their short chemical half-life.
Alan C. Sartorelli - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and evaluation of 1,2,2-tris(sulfonyl)hydrazines as antineoplastic and trypanocidal agents.
Journal of Medicinal Chemistry, 1990Co-Authors: Krishnamurthy Shyam, Curtis L. Patton, Regina Loomis, Philip G. Penketh, Alan A. Divo, Alan C. SartorelliAbstract:Several 1,2,2-tris(sulfonyl) hydrazines, conceived as prodrugs of 1,2-bis (sulfonyl) hydrazines, were synthesized and evaluated for antineoplastic and trypanocidal activities in mice. 1-Methyl-1,2,2-tris (methylsulfonyl) hydrazine emerged as an extremely efficacious antitrypanosomal agent, whereas 1-(2-chloroethyl)-1,2,2-tris(methylsulfonyl) hydrazine was inactive. In contrast, 1-(2-chloroethyl)-1,2,2-tris (methylsulfonyl) hydrasine displayed potent antineoplastic activity, producing several 60-day «cures» of mice bearing leukemia L1210, leukemia P388, or Sarcoma 180. Furthermore, the fact that the tris (sulfonyl) derivatives will not generate isocyanates, which contribute to the host toxicity of nitrosoureas like 1,3-bis (2-chloroethyl)-1-nitrosourea (BCNU), makes them agents of significant promise in trypanosomal and cancer chemitherapy
Yoshida T - One of the best experts on this subject based on the ideXlab platform.
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Isolation and preliminary characterization of ACNU-resistant sublines of rat brain tumors in vivo.
Journal of Neurosurgery, 1992Co-Authors: Yoshida T, Keiji Shimizu, A. Koulousakis, Virginia E. Sturm, E. BeulsAbstract:✓ Two variant cells lines resistant to the nitrosourea derivative ACNU ((1-4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea hydrochloride), namely C6/ACNU and 9L/ACNU, were selected in vivo from rat brain tumors. Stable resistance to ACNU proved to be a characteristic of these cell lines, whether they were grown in vivo or in vitro. These cell lines exhibited a different pattern of cross-resistance to a wide range of chemotherapeutic agents with dissimilar chemical structures and mechanisms of action as compared with that of other ACNU-resistant cell lines established in vitro. Distinct cross-resistance was observed in both the C6/ACNU and 9L/ACNU cell lines to chloroethyl-nitrosoureas such as BCNU (carmustine), CCNU (lomustine), and methyl CCNU and, additionally, to vincristine, vinblastine, Adriamycin (doxorubicin), and arabinosylcytosine, but not to bleomycin, methotrexate, c/s-platinum, and 5-fluorouracil. This might point to a multifactorial mechanism of drug resistance in ACNU-r...
