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1983 (1)
1Author    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