Chemical and Pharmaceutical Bulletin p. 3441 - 3451 (1984)
Update date:2022-08-03
Topics:
Kawai
Akimoto
Kozai
et al.
Several semisynthetic maytansinoids that differ in the structure of the acyl group at the C3 position were prepared by acylation of maytansinol (3) using appropriate carboxylic acids or their active derivatives, and the effects of the compounds on the growth of Tetrahymena pyriformis and the survival of tumor-bearing mice were determined. Among these analogs, the C3 esters having a straight chain aliphatic acyl (11, 12), cycloalkanecarbonyl (18-20) or phenylacetyl group (22), and those having a 2-(N-acetyl-N-methyl)aminohexanoyl (7) or (2-(N-acetyl-N-methyl)aminophenylpropionyl group (8), strongly inhibited the growth of T. pyriformis and exhibited potent activity against B16 melanoma in mice. The potencies were similar to those of maytansine and ansamitocin P-3. The most striking result was the finding that the phenylglycinate (31) was superior to maytansine in terms of its broader effective dose range against ip B16 melanoma and P388 leukemia in mice; however, higher doses of the phenylglycinate were required.
View MoreHuaian Double Win Chemicals Co.,Ltd.
Contact:+86-13511538872
Address:Blk 43,Greenland Century Town,Huaian District, Huaian City,Jiangsu Province,China
website:http://www.easchem.com
Contact:+86-731-89722861 89722891
Address:2/F-4/Bld Colorful Palace, No.605 Changsha Ave, Yuhua Area Changsha Hunan China.
Contact:+(852) 301-98033
Address:Flat C, 23/F, Lucky Plaza, 315-321 Lockhart Road, Wan Chai, Hong Kong
Zhejiang Haizhou Pharmaceutical Co., Ltd.
website:https://www.haizhoupharma.com/
Contact:+86-576-88221016
Address:No. 19, Donghai 5th Avenue, Yanhai Industrial Zone, Linhai, Zhejiang, China
Huzhou City Linghu Xinwang Chemical Co.,Ltd.
Contact:86-572-3948695/3945236
Address:huzhou
Doi:10.1021/ic50207a063
(1980)Doi:10.1246/cl.2003.24
(2003)Doi:10.1016/S0022-328X(00)85875-1
(1979)Doi:10.1021/jo01347a063
(1966)Doi:10.1023/A:1014447700775
(2001)Doi:10.1021/ol049780x
(2004)
