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'Phosphorylated Diaziridines' in keywords
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1983 (1)
1Author    George Sosnovsky, Jan LukszoRequires cookie*
 Title    In the Search for New Anticancer Drugs, III+ Phosphorylated Diaziridine Derivatives  
 Abstract    Several N-diethoxyphosphoryl derivatives 7 of various diaziridines, and compounds 12, 15a, lob, 18 and 20, structurally related to TEPA (la) and spin labeled Thio-TEPA (lc) were synthesized. 0 Me 0 N-P(0Et) 2 HC=NN-p(<]) o / NR ' • 11 f / 1 ? R-O-P-f N —C—R X R N—R CL N "2 Me Me 7: R 1 . R 3 = alkyl 12 15a: R 1 = R 2 =R 3 =Me R 2 =H, alkyl 15b: R' = H,R 2 R 3 =-|CH2|5-N-0 Me Me In three cases, attempts to synthesize phosphorylated diaziridine derivatives resulted in rearrangements to give the corresponding phosphorylated hydrazone derivatives 11 h, Hi and 12. Me 0 CH = NN — P(0Et)j 11 h: x= H 11 i : x = ci 13 C NMR spectroscopy was shown to be a valuable tool in distinguishing between the structures of diaziridine and hydrazone derivatives. The in vivo testing of five representa-tive compounds (7e, 12, 15a, 16 and 20) against murine lymphocytic leukemia P 388 showed a lack of antitumor activity of compounds 7e, 15 a, 16 and 20, and an activity of compound 12 as evidenced by a T/C value of 194 and a % ILS of 94, at a dose of 32 mg/kg. 
  Reference    Z. Naturforsch. 38b, 884—894 (1983); received August 30/December 24 1982 
  Published    1983 
  Keywords    Phosphorylated Diaziridines, Synthesis, Anticancer Drugs, Leukemia P 388 
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 TEI-XML for    default:Reihe_B/38/ZNB-1983-38b-0884.pdf 
 Identifier    ZNB-1983-38b-0884 
 Volume    38