Buck Suzanne B, Huff Jacquelyn K, Himes Richard H, Georg Gunda I
Department of Medicinal Chemistry, University of Kansas, 1251 Wescoe Drive, Lawrence, KS 66045-7582, USA.
J Med Chem. 2004 Jul 1;47(14):3697-9. doi: 10.1021/jm030555f.
Epi-C3-cryptophycin-24, epi-C3-m-chlorobenzyl-cryptophycin-24, and the corresponding styrenes were synthesized and tested in vitro against the MCF-7 and multidrug-resistant MCF-7/ADR breast cancer cell lines and in an in vitro tubulin assembly assay. The results demonstrate that the S configuration at the C3 stereocenter is not required to induce potent cytotoxicity and the m-Cl substituent present on the C10 side chain did not induce any large change in activity.
合成了表- C3 -隐藻素- 24、表- C3 -间氯苄基-隐藻素- 24以及相应的苯乙烯类化合物，并在体外针对MCF - 7和多药耐药的MCF - 7/ADR乳腺癌细胞系进行了测试，还进行了体外微管蛋白组装试验。结果表明，C3立体中心的S构型并非诱导强效细胞毒性所必需的，且C10侧链上存在的间氯取代基并未引起活性的任何显著变化。
