Abstract
Two isomeric aziridine-containing analogs of spermidine, a polyamine, were synthesized and evaluated for cytotoxic activity against cancer cell lines. Replacement of one of the primary amino groups of spermidine with an aziridinyl functionality yielded either N 1-aziridinylspermidine[ N-(3-aziridinylpropyl)-1,4-diaminobutane] or N 8-aziridinylspermidine [ N-(4-aziridinylbutyl)-1,3-diamino-propane]. N 1-Aziridinylspermidine was cytotoxic in vitro against L1210 Murine leukemia cells ( ic 50 0.15 μM) and HL60 human leukemia cells ( IC 50 0.11 μM). N 8-Aziridinylspermidine was slightly less potent against L1210 ( ic 50 0.31 μM) and HL60 ( IC 50 0.30 μM) cells. When screened by the Developmental Therapeutics Program of the National Cancer Institute, these compounds proved cytotoxic against a wide variety of tumor types. Both compounds inhibited incorporation of radiolabeled thymidine, uridine, and valine into trichloroacetic acid-precipitable material by L1210 cells. Aminoguanidine did not affect the potency of the aziridinylspermidines.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
