148892-52-8Relevant articles and documents
Cysteine chloromethyl and diazomethyl ketone derivatives with potent anti-leukemic activity
Perrey, David A.,Narla, Rama Krishna,Uckun, Fatih M.
, p. 547 - 549 (2000)
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 μM against Nalm-6, 2.3 μM against Molt-3) and N-acetyl-S-trans,trans-farnesyl-Cys chloromethyl ketone (IC50 = 3.0 μM against Nalm-6 and 1.4 μM against Molt-3). (C) Elsevier Science Ltd. All rights reserved.
Compounds for inhibition of proteolysis
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, (2008/06/13)
Compounds used to treat cancer which inhibit carboxy terminal proteolysis of proteins having a carboxyl-terminal -CAAX motif (C=cysteine, A=aliphatic amino acid, and X=any amino acid). The compounds have the formula W--Y--CH2 --Q, where: PA1 1) W is a substituted or unsubstituted farnesyl group, a substituted or unsubstituted geranylgeranyl group, or a lipophilic alkyl, alkenyl, aryl or arylalkyl hydrocarbon group; PA1 2) Y is: STR1 wherein T1 is: --H, --CH3, --F, or --(CH2)n --X1 ; in which n is an integer 20; and X1 is: --SH, --COOH, or --CONH2 ; PA1 T2 is: --N-benzxyloxycarbonyl (Boc), N--φ--, in which φ is an amino acid or a polypeptide reside; and STR2 wherein X2 is a peptide residue linked to carbon via the amino terminal nitrogen; and X3 is a peptide residue linked via an alpha carbon of the peptide; n is an integer 20, X4 is a halide and β is an amino acid residue. -GOVT PAR This invention was supported by Grant No. EY03624 and the government has certain rights to the invention.