Journal of Medicinal Chemistry p. 1450 - 1455 (1981)
Update date:2022-08-05
Topics:
Rosowsky, Andre
Forsch, Ronald
Uren, Jack
Wick, Michael
The γ-tert-butyl ester (1), γ-hydrazide (2), γ-n-butylamide (3), and γ-benzylamide (4) derivatives of methotrexate (MTX) were synthesized from 4-amino-4-deoxy-N10-methylpteroic acid (APA) and the appropriate blocked L-glutamic acid precursors with the aid of the peptide bond forming reagent diethyl phosphorocyanidate.The affinity of these side chain modified products for dihydrofolate reductase (DHFR) from Lactobacillus casei and L1210 mouse leukemic cells was determined spectrophotometrically or by competitive radioligand binding assay, and their cytotoxicity was evaluated against L1210 leukemic cells in culture.The results provide continuing support for the view that the "γ-terminal region" of the MTX side chain is an attractive site for molecular modification of this anticancer agent.
View MoreChongqing Werlchem Fine Chemical Co. Ltd
Contact:+86-23-67521957
Address:NO.15,Fortune Road,Yubei District,401121,Chongqing,China
AstaTech ( Chengdu) BioPharmaceutical Corp.
website:http://www.astabiochem.cn/
Contact:+86-15198215156-15198215156
Address:SICHUAN CHENGDU
Weifang Adde Economic And Trade Co.,LTD.
Contact:86-536-8885548
Address:Room 1402,Wanda Plaza B Block,No.958,Yuanfei Road,Kuiwen District
Yingkou Sanzheng Organic Chemical Co. Ltd.
Contact:+86-417-3638818
Address:25 Gengxinli Village, Daqing Road, Yingkou, Liaoning, China
FOSHAN NANHAI ZHONGNAN PHARMACEUTICAL FACTORY
Contact:0086-0757-85609331
Address:XIAHENGTIAN INDUSTRIAL ZONE,SHAYONG VILLAGE,LISHUI TOWN
Doi:10.1021/j100192a018
(1992)Doi:10.1016/j.apcata.2012.03.009
(2012)Doi:10.1021/acs.inorgchem.1c01488
(2021)Doi:10.1016/S0968-0896(00)00310-2
(2001)Doi:10.1039/c39810000698
(1981)Doi:10.1007/BF00505608
(1981)