title: Hybrid aza-steroid alkylators in the treatment of colon cancer.
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.
authors.affiliation: 1st Department of Medical Oncology, Metaxa Cancer Hospital, Piraeus, Greece. dtrafalis@yahoo.com <dtrafalis@yahoo.com>
authors.forename: Dimitrios T P
authors.initials: DT
authors.lastname: Trafalis
mesh_terms: D000477:Alkylating Agents / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001378:Azasteroids / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D004305:Dose-Response Relationship, Drug; D005260:Female; D019073:HT29 Cells; D006801:Humans; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008811:Mice, Inbred DBA; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000473:pathology; D009588:Nitrogen Mustard Compounds / Q000737:chemistry / Q000494:pharmacology*; D012632:Secosteroids / Q000737:chemistry / Q000494:pharmacology*; D013997:Time Factors; D023041:Xenograft Model Antitumor Assays
chemical_list: C515329:3-hydroxy-13-amino-13,17-secoandrostan-17-oic-13,17-lactam p-bis(2-chloroethyl)amino phenyl acetate; C515882:3-hydroxy-3-aza-A-homoandrosten-4-one-4-bis(2-chloroethyl)aminophenoxyacetate; D000477:Alkylating Agents; D001378:Azasteroids; D009588:Nitrogen Mustard Compounds; D012632:Secosteroids