Cancer Letters
Volume 243, Issue 2 , Pages 202-210, 18 November 2006

Hybrid aza-steroid alkylators in the treatment of colon cancer

  • Dimitrios T.P. Trafalis

      Affiliations

    • 1st Department of Medical Oncology, ‘Metaxa’ Cancer Hospital, Piraeus, Greece
    • Laboratory of Medicinal Chemistry, Faculty of Pharmacy, University of Patras, Greece
    • Corresponding Author InformationPresent address: 1st Department of Medical Oncology, ‘Metaxa’ Cancer Hospital, 15 Larnakos, 17341 Agios Dimitrios, Athens, Greece. Tel.: +30 210 971 5465; fax: +30 210 971 3766.

Received 15 October 2005; received in revised form 4 November 2005; accepted 27 November 2005.

Abstract 

We tested two alkylating homo-aza-steroid esters, lactandrate and lactestoxate, for antineoplastic activity against colon adenocarcinoma in vitro and in vivo. Cytostatic and cytotoxic activity was evaluated in vitro with the SRB colormetric assay against nine human colon adenocarcinoma cell lines. The in vivo anti-tumour effect was determined against two rodent colon carcinomas, the Colon 26 and the relatively chemoresistant Colon 38 carcinoma, as well as against the human xenograft CX-1 colon carcinoma. Both of the tested compounds displayed a very satisfactory anti-cancer activity in vitro and in vivo. Lactestoxate produced a significantly higher overall activity than lactandrate.

Keywords: Colon carcinoma, Human cell lines, Homo-aza-steroids, Lactam steroid alkylator, In vitro, In vivo

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PII: S0304-3835(05)01043-8

doi:10.1016/j.canlet.2005.11.034

Cancer Letters
Volume 243, Issue 2 , Pages 202-210, 18 November 2006

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