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Cysteine chloromethyl and diazomethyl ketone derivatives with potent anti-leukemic activity.

Abstract：

:A series of cysteine diazomethyl- and chloromethyl ketone derivatives has been synthesized and evaluated against human B-lineage (Nalm-6) and T-lineage (Molt-3) acute lymphoblastic leukemia cell lines. The chloromethyl ketone compounds showed potent cytotoxicity against these cell lines, with IC50 values in the low micromolar range. The best compounds were N-acetyl-S-dodecyl-Cys chloromethyl ketone (IC50 = 2.0 microM against Nalm-6, 2.3 microM against Molt-3) and N-acetyl-S-trans,trans-farnesyl-Cys chloromethyl ketone (IC50 = 3.0 microM against Nalm-6 and 1.4 microM against Molt-3).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Perrey DA,Narla RK,Uckun FM

doi

10.1016/s0960-894x(00)00046-9

subject

Has Abstract

pub_date

2000-03-20 00:00:00

pages

547-9

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(00)00046-9

journal_volume

10

pub_type

杂志文章

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