ANTITUMOR AND CYTOGENETIC EFFECTS OF ESTERIC (ASE) AND AMIDIC (ASA) STEROIDAL DERIVATIVE OF P-BIS (2-CHLOROETHYL) AMINO PHENYLACETIC ACID (CAPA) - A COMPARATIVE-STUDY
Ss. Nikolaropoulos et al., ANTITUMOR AND CYTOGENETIC EFFECTS OF ESTERIC (ASE) AND AMIDIC (ASA) STEROIDAL DERIVATIVE OF P-BIS (2-CHLOROETHYL) AMINO PHENYLACETIC ACID (CAPA) - A COMPARATIVE-STUDY, Anticancer research, 17(6D), 1997, pp. 4525-4529
The homo-aza-steroidal ester of p-bis (2-chloroethyl) amino phenylacet
ic acid (ASE) (I), the homo-aza-steroidal amide of p-bis (2-chloroethy
l) amino phenylacetic acid (ASA) (II), and the parent compound p-bis (
2-chloroethyl) amino phenylacetic acid (III) were tested in an effort
to evaluate their ability to inhibit a transplanted leukemia (P388) in
vivo, and the DNA synthesis of P388 cell cultures in vitro. The compo
unds' effects on Sister Chromatid Exchange (SCE) rate and on human cel
l proliferation kinetics in vitro were also studied. The above mention
ed compounds were identified as displaying cytogenetic, cytostatic and
antineoplastic effects, the ester compound being the more potent. The
main conclusion from this study is that the existence of the esteric
bond is necessary for the expression of the antitumor activity. The sy
nthetic route for the preparation of the amidic derivative (II), as ne
w product, is also reported.