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Synthesis and SAR of vinca alkaloid analogues |
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| Authors: | Matthew E Voss Jeffery M Ralph Dejian Xie David D Manning Xinchao Chen Anthony J Frank Andrew J Leyhane Lei Liu Jason M Stevens Cheryl Budde Matthew D Surman Thomas Friedrich Denise Peace Ian L Scott Mark Wolf Randall Johnson |
| Institution: | 1. Albany Molecular Research, Inc., 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA;2. Albany Molecular Research, Inc., 7001 Performance Drive, North Syracuse, NY 13212, USA;3. Albany Medical College, 43 New Scotland Avenue, Albany, NY 12208, USA;4. 1104 Piedras Rajas, Santa Fe, NM 87501, USA |
| Abstract: | Versatile intermediates 12′-iodovinblastine, 12′-iodovincristine and 11′-iodovinorelbine were utilized as substrates for transition metal based chemistry which led to the preparation of novel analogues of the vinca alkaloids. The synthesis of key iodo intermediates, their transformation into final products, and the SAR based upon HeLa and MCF-7 cell toxicity assays is presented. Selected analogues 27 and 36 show promising anticancer activity in the P388 murine leukemia model. |
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