Antitumor and anti-Pneumocystis carinii activities of novel bisbenzamidines

Jean Jacques Vanden Eynde, Annie Mayence, Melissa T. Johnson, Tien L. Huang, Margaret S. Collins, Sandra Rebholz, Peter D. Walzer, Melanie T. Cushion, Isaac O. Donkor

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Among a library of 17 bisbenzamidines connected with various linkers, compounds with a flexible pentanediamide (10) or hexanediamide (12) linker were the most potent derivatives against rat Pneumocystis carinii (IC50 values of 3 and 2 nM, respectively) and had the highest selectivity index ratios (GI50 of human tumor cells/IC50 of rat P. carinii cells) of >104. Seven compounds caused 50% growth inhibition (GI 50) of tumor cells at concentrations of <100 μM while the remaining ten were not cytotoxic. DNA binding affinity (ΔTm) of the tested compounds did not correlate with either their anti-P. carinii activity or cytotoxicity.

Original languageEnglish (US)
Pages (from-to)143-157
Number of pages15
JournalMedicinal Chemistry Research
Volume14
Issue number3
DOIs
StatePublished - Dec 1 2005

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Pneumocystis carinii
Rats
Tumors
Cells
Inhibitory Concentration 50
Cytotoxicity
Derivatives
Libraries
DNA
Neoplasms
Growth

All Science Journal Classification (ASJC) codes

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

Cite this

Vanden Eynde, J. J., Mayence, A., Johnson, M. T., Huang, T. L., Collins, M. S., Rebholz, S., ... Donkor, I. O. (2005). Antitumor and anti-Pneumocystis carinii activities of novel bisbenzamidines. Medicinal Chemistry Research, 14(3), 143-157. https://doi.org/10.1007/s00044-005-0130-2

Antitumor and anti-Pneumocystis carinii activities of novel bisbenzamidines. / Vanden Eynde, Jean Jacques; Mayence, Annie; Johnson, Melissa T.; Huang, Tien L.; Collins, Margaret S.; Rebholz, Sandra; Walzer, Peter D.; Cushion, Melanie T.; Donkor, Isaac O.

In: Medicinal Chemistry Research, Vol. 14, No. 3, 01.12.2005, p. 143-157.

Research output: Contribution to journalArticle

Vanden Eynde, JJ, Mayence, A, Johnson, MT, Huang, TL, Collins, MS, Rebholz, S, Walzer, PD, Cushion, MT & Donkor, IO 2005, 'Antitumor and anti-Pneumocystis carinii activities of novel bisbenzamidines', Medicinal Chemistry Research, vol. 14, no. 3, pp. 143-157. https://doi.org/10.1007/s00044-005-0130-2
Vanden Eynde JJ, Mayence A, Johnson MT, Huang TL, Collins MS, Rebholz S et al. Antitumor and anti-Pneumocystis carinii activities of novel bisbenzamidines. Medicinal Chemistry Research. 2005 Dec 1;14(3):143-157. https://doi.org/10.1007/s00044-005-0130-2
Vanden Eynde, Jean Jacques ; Mayence, Annie ; Johnson, Melissa T. ; Huang, Tien L. ; Collins, Margaret S. ; Rebholz, Sandra ; Walzer, Peter D. ; Cushion, Melanie T. ; Donkor, Isaac O. / Antitumor and anti-Pneumocystis carinii activities of novel bisbenzamidines. In: Medicinal Chemistry Research. 2005 ; Vol. 14, No. 3. pp. 143-157.
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