Cell specific cytotoxicity and structure-activity relationship of lipophilic 1-B-D-arabinofuranosylcytosine (ara-C) derivatives. |
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| Authors: | G J Peters D A Voorn C M Kuiper C L van der Wilt P Noordhuis K Smid F Myhren M Sandvold H R Hendriks |
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| Institution: | Dept. Oncology, University Hospital VU, Amsterdam. |
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| Abstract: | Lipophilic derivatives of ara-C were developed with the aim to improve drug penetration and retention in solid tumors. Ara-C was esterified at the 5'-position with fatty acids (16-22 C-atoms, 0-3 double bonds). The derivatives were inactive in cell lines with various forms of ara-C and 2',2'-difluorodeoxycytidine (dFdC, gemcitabine) resistance, including deoxycytidine kinase (dCK) deficiency. The activity in the parent cell lines correlated negatively with chain length and positively with double bonds. |
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