Synthesis and bioevaluation of a series of fatty acid esters of p-[N,N-bis(2-chloroethyl)amino]phenol.

Abstract:

:A series of even numbered fatty acid esters (C2-C18) of p-[N,N-bis(2-chloroethyl)amino]phenol were synthesized and evaluated as to acute toxicity as well as effectiveness against L-1210 mouse leukemia. The acetate through the decanoate derivatives demonstrated toxicity between 2 and 3 times that of phenol mustard in HA/ICR mice. The less soluble laurate, myristate, palmitate, and stearate derivatives were less toxic. Significant survival times in the leukemia studies (T/C% greater than or equal to 125) were observed for all compounds except the acetate and hexanoate derivatives. The myristate derivative produced the greatest significant increase in survival time, 162%. The palmitate and stearate derivatives produced significant survival at five and four dosage levels, respectively. The butyrate and laurate derivatives produced significant survival at three dosage levels and the octanoate, decanoate, and myristate at two dosage levels.

journal_name

J Pharm Sci

authors

Wynn JE,Caldwell ML,Robinson JR,Beamer RL,Bauguess CT

doi

10.1002/jps.2600710713

subject

Has Abstract

pub_date

1982-07-01 00:00:00

pages

772-6

issue

7

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)44239-X

journal_volume

71

pub_type

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