Synthesis and antitumor activity of novel C-8 ester derivatives of leinamycin |
| |
Authors: | Kanda Yutaka Ashizawa Tadashi Kawashima Kenji Ikeda Shun-ichi Tamaoki Tatsuya |
| |
Affiliation: | Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd., 1188 Shimotogari, Nagaizumi-cho, Sunto-gun, Shizuoka 411-8731, Japan. ykanda@kyowa.co.jp |
| |
Abstract: | A novel series of C-8 ester derivatives of leinamycin are described. Condensation of N-substituted amino acids or carboxylic acids containing polyether moiety with leinamycin resulted in the C-8 ester derivatives with good antitumor activity in several experimental models. Among these derivatives, compound 4e, which has five ethylene glycol ether units in the C-8 acyl group, showed potent antitumor activity against human tumor xenograft. Combination with the modification of the dithiolanone moiety was applied to these C-8 ester derivatives and some of them also showed good antitumor activity. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|