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Research ArticleExperimental Studies

Abilities of 3,4-Diarylfuran-2-one Analogs of Combretastatin A-4 to Inhibit Both Proliferation of Tumor Cell Lines and Growth of Relevant Tumors in Nude Mice

LICHUN SUN, NATALYA I. VASILEVICH, JOSEPH A. FUSELIER and DAVID H. COY
Anticancer Research January 2004, 24 (1) 179-186;
LICHUN SUN
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NATALYA I. VASILEVICH
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JOSEPH A. FUSELIER
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DAVID H. COY
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Abstract

Background: Combretastatin A-4 (CA-4) and its analogs are potent inhibitors of tubulin polymerization and display strong inhibitory activity on both solid tumor and tumor cell growth. Since natural CA-4 is difficult to synthesize and also isomerizes to an inactive form quite readily, a recently reported new 3,4-diarylfuran-2-one-based series of CA-4 analogs was investigated, in the hope of bypassing some of these difficulties. These analogs appear to offer a valuable tool for CA-4 research because of their extremely facile synthesis from readily available starting materials. Materials and Methods: The CA-4 analogs were evaluated by MTT assay, cell cycle analysis, tubulin polymerization and tumor-inhibiting experiments. Results: Various benzene ring substitutions on the furan-2-one skeleton (analogs to the two aromatic rings on the CA-4 styrene skeleton) quickly demonstrated that the structure-activity relationships are quite similar to previously synthesized CA-4 analogs. The most interesting analog appears to be an anilino compound (NV-5-9) which was also quite soluble. Analog NV-5-9 was remarkably potent in all tested tumor cell lines and could strongly inhibit tubulin polymerization at doses as low as 1 mM. Further experiments with tumor-bearing mice indicated that NV-5-9 and other potent analogs (NV-4-82 and NV-4-86) were effective in treating human prostate PC-3 and SCLC NCI-H69 tumors at well below an oral MTD dose of around 200 mg/kg body weight. This suggests some bioavailability by this route. Conclusion: These data strongly support that NV-5-9 is extremely potent, readily synthesizable and apparently suitable for in vivo studies employing transplanted tumors.

  • Received August 7, 2003.
  • Accepted December 16, 2003.
  • Copyright© 2004 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved
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Anticancer Research: 24 (1)
Anticancer Research
Vol. 24, Issue 1
January-February 2004
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Abilities of 3,4-Diarylfuran-2-one Analogs of Combretastatin A-4 to Inhibit Both Proliferation of Tumor Cell Lines and Growth of Relevant Tumors in Nude Mice
LICHUN SUN, NATALYA I. VASILEVICH, JOSEPH A. FUSELIER, DAVID H. COY
Anticancer Research Jan 2004, 24 (1) 179-186;

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Abilities of 3,4-Diarylfuran-2-one Analogs of Combretastatin A-4 to Inhibit Both Proliferation of Tumor Cell Lines and Growth of Relevant Tumors in Nude Mice
LICHUN SUN, NATALYA I. VASILEVICH, JOSEPH A. FUSELIER, DAVID H. COY
Anticancer Research Jan 2004, 24 (1) 179-186;
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