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1983 (2)
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 
2Author    George Sosnovsky, BuddhaD. PaulRequires cookie*
 Title    In the Search for New Anticancer Drugs, VI+ Structural Modifications of Cyclophosphamide  
 Abstract    Taking into consideration the known mechanism of the drug action of cyclophosphamide (1), several analogs and related compounds o, 6, 7, 9, 11, 12 and 27 were synthesized, and tested against lymphocytic leukemia P 388 in mice. CH °N P(0)NM2 (P(0)NM2 F /P(0)NM2 F ,P(0)NM2 I H3cV N 'H h>\ H CH 3 3 CH3 3 CH3 M=CH2CH2CI 5 6 7 (>™2 HO<3-P,O,NM2 / \ R HiC ' w o ' P-NCHUCHUCL 9 11, R = CI 12 27, r^nhch2CH2CH3 Moderate to high activity was found with 5 (T/C X 100 = 243 at a dose of 300 mg/kg), 7 (T/C x 100 = 173 at a dose of 10 mg/kg), 9 (T/C X 100 = 248 at a dose of 100 mg/kg) and 11 (T/C X 100 = 155 at a dose of 55 mg/kg). None of these compounds was found to be more active than 1 (T/C X 100 = 339 at a dose of 65 mg/kg). Although the essential position C4 for the enzymatic activation is completely blocked in 5, the compound posses-ses a high degree of activity. This result justifies a reevaluation of the proposed mechanism of drug action of 1 and its analogs. 
  Reference    Z. Naturforsch. 38b, 1146—1155 (1983); received August 30/December 24 1982 
  Published    1983 
  Keywords    Cyclophosphamide, Drugs, Anticancer, Synthesis, Leukemia P 388 
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 TEI-XML for    default:Reihe_B/38/ZNB-1983-38b-1146.pdf 
 Identifier    ZNB-1983-38b-1146 
 Volume    38