adozelesin and Carcinoma--Squamous-Cell

adozelesin has been researched along with Carcinoma--Squamous-Cell* in 2 studies

Other Studies

2 other study(ies) available for adozelesin and Carcinoma--Squamous-Cell

ArticleYear
Total synthesis and biological properties of novel antineoplastic (chloromethyl)furanoindolines: an asymmetric hydroboration mediated synthesis of the alkylation subunits.
    Journal of medicinal chemistry, 1994, Jan-21, Volume: 37, Issue:2

    1,2-Dihydro-1-(chloromethyl)-5-hydroxy-8-methyl-3H-furano[3,2-e]in dole (CFI) as a novel replacement of the cyclopropylpyrroloindoline (CPI) alkylation subunit of CC-1065, U-71184, and U-73975 (adozelesin) has been synthesized and incorporated into a series of efficacious antineoplastic agents. A partial solution to an asymmetric synthesis of the CFI alkylation subunit has been achieved by the implementation of an asymmetric hydroboration reaction of an intermediate 3-methyleneindoline (13). Extension to the asymmetric synthesis of the CBI and CI alkylation subunits is presented. The demonstration and comparative study of the sequence-selective DNA alkylation properties of the CFI-based agents are detailed, and the preliminary in vitro and in vivo antineoplastic properties of these agents in the human epidermoid cell lung carcinoma (T222) are described.

    Topics: Alkylation; Animals; Antineoplastic Agents; Base Sequence; Benzofurans; Boron Compounds; Carcinoma, Squamous Cell; Cyclohexanecarboxylic Acids; Cyclohexenes; DNA; Drug Screening Assays, Antitumor; Duocarmycins; Female; Furans; Humans; Indoles; Leucomycins; Lung Neoplasms; Mice; Mice, Nude; Molecular Sequence Data; Tumor Cells, Cultured

1994
Evaluation of the antineoplastic activity of adozelesin alone and in combination with 5-aza-2'-deoxycytidine and cytosine arabinoside on DLD-1 human colon carcinoma cells.
    Anti-cancer drugs, 1993, Volume: 4, Issue:3

    Adozelesin (Ado), a CC-1065 analog, shows significant antineoplastic activity in vivo against several types of murine tumors and human tumor xenografts. Ado is a DNA alkylating agent. One objective of this study was to investigate the cytotoxic action of Ado against the human colon (HT-29, DLD-1) and the lung (SK) carcinoma cell lines. The concentrations of Ado that produced 50% cell kill for a 4 and 24 h exposure were in the range of 0.001-0.02 ng/ml for both colon and lung carcinoma cells, indicating that this analog was a very potent cytotoxic agent. Since most clinical regimens for tumor therapy consist of several drugs, we investigated the antineoplastic action of Ado in combination with 5-aza-2'-deoxycytidine (5-Aza-CdR), a potent inhibitor of DNA methylation or cytosine arabinoside (Ara-C), a potent inhibitor of DNA synthesis. The Ado plus 5-Aza-CdR combination showed a synergistic effect on cytotoxicity of DLD-1 colon carcinoma cells for both a 6 and 24 h exposure. However, combination of Ado and Ara-C for a 6 h exposure showed an antagonistic effect, whereas a 24 h exposure showed a synergistic effect. These preclinical results provide some preliminary data on possible drugs that can be selected for use in combination with Ado in future clinical trials in patients with cancer.

    Topics: Adenocarcinoma; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Azacitidine; Benzofurans; Carcinoma, Squamous Cell; Cell Division; Colonic Neoplasms; Cyclohexanecarboxylic Acids; Cyclohexenes; Cytarabine; Decitabine; DNA, Neoplasm; Drug Screening Assays, Antitumor; Duocarmycins; Humans; Indoles; Lung Neoplasms; Time Factors; Tumor Cells, Cultured

1993