Dichloroethyl carbamoyl ester of delta-9-tetrahydrocannabinol. Chemical synthesis and biological testing and evaluation as a potentially site-specific anti-tumor agent.
A novel compound, Delta-9-Tetrahydrocannabinol Nitrogen Mustard (THC-mustard), was chemically synthesized and characterized. The rationale was to target a known anti-tumor agent, nitrogen mustard, to tumor cells with "THC Receptors" and/or "Estrogen Receptors". A microtest in vitro bioassay was designed and developed to compare the ID50 of the drug in cell culture against various tumor cell types. The ID50's of the THC-mustard were determined against several tumor cell types in culture, compared with Mechlorethamine HCl, Delta-9-Tetrahydrocannabinol (THC), and an equimolar mixture of THC and nitrogen mustard. A preliminary toxicity study by the NCI of the THC-mustard (in vivo) in Swiss male mice bearing the P388 tumor (1 dose X 1 day) by the I.P. route was also carried out. A description of the rationale, chemical synthesis and characterization, bioassay, and results is herewith presented.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000627:therapeutic use*; D002478:Cells, Cultured; D013759:Dronabinol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004357:Drug Synergism; D008466:Mechlorethamine / Q000008:administration & dosage / Q000494:pharmacology*; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy; D009588:Nitrogen Mustard Compounds / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats
D000970:Antineoplastic Agents; D009588:Nitrogen Mustard Compounds; D008466:Mechlorethamine; D013759:Dronabinol; C044394:delta-9-tetrahydrocannabinol dichloroethyl carbamoyl ester