Chemical and Pharmaceutical Bulletin p. 310 - 313 (1993)
Update date:2022-08-04
Topics:
Sawada
Yaegashi
Furuta
Yokokura
Miyasaka
7-Ethylcamptothecin (1d), a model which does not have any site on the A-ring for further modification was converted into water-soluble derivatives by opening the E-ring lactone. 1d was heated in N,N-dimethylenediamine to yield amide 2a, and this was then acylated to furnish 3a-q, which were soluble in water as their HCl salts. The propionyl (3b), butyryl (3c) and methylthiopropionyl (3h) derivatives showed higher activity than the sodium salt of 1d. The acyl group makes the derivatives more lipophilic, and ease of hydrolysis of amide 2a to 1d is thought to be necessary for significant activity.
Contact:86-21-34622192，13917187091，21-34622765
Address:No. 500 Caobao Road Shanghai P.R China
Neworld Chemical Co., Ltd Shanghai(expird)
Contact:+86-21-62202658
Address:11F, Blvd 2, No. 1969 PuXing Rd, Shanghai
Landz International Company Ltd.
Contact:0086-21-58891610
Address:985 Dongfang Road, Pudong, Shanghai 200122 China
Improve Medical Technology(Nanxiong) Co., Ltd
Contact:86-751-3836997
Address:No.33, Pingan First Road, Fine Chemical Industry Base, Nanxiong City, Shaoguan, Guangdong, China
Tianjin Bright Future Technology Co., Ltd
Contact:0086-22-58016666
Address:NO.136 DongTeng Lake Street Tianjin Economic and Technology Development Area,Tainjin,China
Doi:10.1016/j.tetlet.2018.05.010
(2018)Doi:10.1021/jm00127a015
(1989)Doi:10.1021/jo902477n
(2010)Doi:10.1055/s-1989-27148
(1989)Doi:10.1016/S0040-4020(01)81443-5
(1988)Doi:10.1021/ja902140m
(2009)
