Synthesis, evaluation of chemical reactivity, and murine antineoplastic activity of 2-hydroxy-5-(3, 4-dichlorophenyl)-6, 7-bis (hydroxymethyl)-2, 3-dihydro-1H- …

…, CP Chang, HL McPherson Jr

Index: Anderson, Wayne K.; Chang, Chiung-Pin; McPherson, Howard L. Journal of Medicinal Chemistry, 1983 , vol. 26, # 9 p. 1333 - 1338

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Citation Number: 20

Abstract

2-Hydroxy-5-(3, 4-dichlorophenyl)-6, 7-bis (hydroxymethyl)-2, 3-dihydro-1H-pyrrolizine bis (2-propylcarbamate)(1 1) was prepared in a multistep synthesis. The 2-hydroxy group was used to prepare ester prodrugs 14 and 15, and the antineoplastic activities of 11, 14, and 15a were compared to 1 (the 2-deoxy analogue of 11) in murine P388 lymphocytic leukemia and B16 melanocarcinoma. The alcohol 11 showed comparable activity to 1, while 14 was ...

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