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. 2003 Jun 21;1(12):2120-36.
doi: 10.1039/b209990j.

Syntheses and biological evaluation of vinblastine congeners

Martin E Kuehne  1 , William G Bornmann, Istvan Markó, Yong Qin, Karen L LeBoulluec, Deborah A Frasier, Feng Xu, Tshilundu Mulamba, Carol L Ensinger, Linda S Borman, Anne E Huot, Christopher Exon, Fred T Bizzarro, Julia B Cheung, Susan L Bane
Affiliations

Syntheses and biological evaluation of vinblastine congeners

Martin E Kuehne et al. Org Biomol Chem. .

Erratum in

  • Org Biomol Chem. 2003 Jul 7;1(13):2403

Abstract

Sixty-two congeners of vinblastine (VLB), primarily with modifications of the piperidine ring in the carbomethoxycleavamine moiety of the binary alkaloid, were synthesized and evaluated for cytotoxicity against murine L1210 leukemia and RCC-2 rat colon cancer cells, and for their ability to inhibit polymerization of microtubular protein at < 10(-6) M, and for induction of spiralization of microtubular protein, and for microtubular disassembly at 10(-4) M concentrations. An ID50 range of >10(7) M concentrations was found for L1210 inhibition by these compounds, with the most active 1000x as potent as vinblastine.

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