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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

The Disulfide Analogues of Isophosphoramide Mustard for Anticancer Therapy

Author(s): Joanna Cytarska, Krzysztof Skowerski, Szymon Jaworski, Konrad Misiura, Beata Filip-Psurska and Joanna Wietrzyk

Volume 12, Issue 3, 2015

Page: [172 - 179] Pages: 8

DOI: 10.2174/1570180811666141010001007

Price: $65

Abstract

Novel disulfide analogues of isophosphoramide mustard (iPAM) were designed and synthesised. All compounds were hydrolytically stable and underwent reduction by L-glutathione with different kinetic parameters. Based on the HPLC-MS analysis a mechanism of activation by glutathione obtained disulfide analogues of iPAM was proposed. The compounds were tested for cytotoxic activity against human promyelocytic leukaemia HL-60, human lymphoblastic leukaemia MOLT-4, human lymphoblastic leukaemia CCRF/CEM, human bladder cancer HCV29T, murine melanoma B16-F0 and murine fibroblasts Balb3T3 cell lines. The most promising anticancer activity was exhibited by compound 4, which proved to be more active than the reference cisplatin against all cancer cell lines.

Keywords: Anticancer activity, disulfide, glutathione, isophosphoramide mustard.

Graphical Abstract


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