2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate:: A potent antitumor agent

被引：7

作者：

Huang, ZH

Yang, GJ

Lin, ZL

Huang, JL ^{[1
]}

机构：

[1] Fudan Univ, Dept Macromol Sci, Educ Minist China, Key Lab Mol Engn Polymers, Shanghai 200433, Peoples R China

[2] Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(01)00157-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-[N-1-2-Pyrimidyl-aminobenzensulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate has been prepared by reaction of chlorambucil with sulfadiazine derivative. Schiff's base has been used as the protective group of the;aromatic amine in the synthesis. It can be completely removed by the irradiation of 365 nm UV light at room temperature. The title compound exhibits a high antitumor activity with a therapeutic index (TI) of 47.55 which is twice that of chlorambucil's (TI: 22.84). (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1099 / 1103

页数：5

共 50 条

[1] 2-[4-BIS(2-CHLOROETHYL)AMINOPHENYL]INDANE-1,3-DIONE AND ITS DEHYDRODIMER
NIKULIN, VI
PISARENKO, LM
[J]. BULLETIN OF THE ACADEMY OF SCIENCES OF THE USSR DIVISION OF CHEMICAL SCIENCE, 1990, 39 (04): : 848 - 850
[2] POTENTIAL ANTITUMOR AGENT DICYCLOHEXYLAMMONIUM 2-[4-[N,N-BIS(2-CHLOROETHYL)AMINO]-2-METHYLPROPIONATE
SOMMER, HZ
WICKS, GE
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1972, 15 (04) : 436 - &
[3] Discovery of N-(2-Aminophenyl)-4-(bis(2-chloroethyl)amino) Benzamide as a Potent Histone Deacetylase Inhibitor
Zhang, Lihui
Lin, Xiaoyang
Chen, Yiming
Wan, Minghui
Jiang, Qixiao
Zhang, Li
Chou, C. James
Song, Weiguo
Zhang, Lei
[J]. FRONTIERS IN PHARMACOLOGY, 2019, 10
[4] ANTITUMOR AGENT 1,3-BIS(2-CHLOROETHYL)-1-NITROSOUREA
LOO, TI
DION, RL
DIXON, RL
RALL, PD
[J]. JOURNAL OF PHARMACEUTICAL SCIENCES, 1966, 55 (05) : 492 - &
[5] Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines
Shyam, K
Penketh, PG
Loomis, RH
Rose, WC
Sartorelli, AC
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (03) : 796 - 801
[6] 5-BIS-(2-CHLOROETHYL)-AMINOURACIL, A NEW ANTITUMOR AGENT
LYTTLE, DA
PETERING, HG
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1958, 80 (23) : 6459 - 6460
[7] Structural characterization and nonlinear optical properties of 1-phenyl-3-(4-bis(2-chloroethyl)aminophenyl)-2-propen-1-one
Sankaraperumal, Anitha
Shetty, A. N.
Karthikeyan, J.
[J]. JOURNAL OF STRUCTURAL CHEMISTRY, 2015, 56 (07) : 1398 - 1404
[8] Structural characterization and nonlinear optical properties of 1-phenyl-3-(4-bis(2-chloroethyl)aminophenyl)-2-propen-1-one
Anitha Sankaraperumal
A. N. Shetty
J. Karthikeyan
[J]. Journal of Structural Chemistry, 2015, 56 : 1398 - 1404
[9] HEXAHYDROPYRIMIDINES .4. SYNTHESIS OF 2-(4-)N,N-BIS)2-CHLOROETHYL)AMINO)ARYL)-1,3-BIS-)ARALKYL)HEXAHYDROPYRIMIDINES AS ANTITUMOR AGENTS
BILLMAN, JH
MEISENHEIMER, JL
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1964, 7 (01) : 115 - &
[10] Synthesis and elucidation of 4-bis(2-chloroethyl)amino-L-phenylalanine
Ashnagar, A.
Naseri, N. Gharib
Darakhshanmehr, M.
[J]. ASIAN JOURNAL OF CHEMISTRY, 2007, 19 (07) : 5399 - 5406

← 1 2 3 4 5 →