Thieno[2,3-d]pyrimidines in the Synthesis of Antitumor and Antioxidant Agents

被引：30

作者：

Aly, Ashraf A. ^{[1
]}

Brown, Alan B. ^{[2
]}

Ramadan, Mohamed ^{[3
]}

Gamal-Eldeen, Amira M. ^{[4
]}

Abdel-Aziz, Mohamed ^{[3
]}

Abuo-Rahma, Gamal El-Din A. A. ^{[3
]}

Radwan, Mohamed F. ^{[3
]}

机构：

[1] Menia Univ, Fac Sci, Dept Chem, El Minia 61519, Egypt

[2] Florida Inst Technol, Dept Chem, Melbourne, FL 32901 USA

[3] Menia Univ, Fac Pharm, Dept Med Chem, El Minia 61519, Egypt

[4] Natl Res Ctr, Dept Biochem, Div Genet Engn & Biotechnol, Giza, Egypt

来源：

ARCHIV DER PHARMAZIE | 2010年 / 343卷 / 05期

基金：

美国国家科学基金会;

关键词：

Antitumor activity; Cyclization; Dimethyl acetylenedicarboxylate; E-Dibenzoylethylene; Thienopyrimidines; PHARMACOLOGICAL ACTIVITIES; ACID-DERIVATIVES; PYRIMIDINES; GROWTH;

D O I：

10.1002/ardp.200900245

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Dimethyl acetylenedicarboxylate, ethyl propiolate, and E-dibenzoylethylene react with thieno-pyrimidines (cyclo-pentyl, -hexyl, and -heptyl) derivatives to form thiazolo[3,2-a]thieno-[2,3-d]pyrimidin-2-ylidene) acetates, thieno[2,3-d]pyrimidin-2-ylthioacrylates, and thieno[2',3':4,5[pyrimido[2,1-b][1,3]thiazin-6-ones, respectively. Reactions proceed via cyclization and thio-addition processes. Some derivatives of thienopyrimidines showed high inhibition of Hep-G2 cell growth compared with the growth of untreated control cells. However, the fused heptyl of thienopyrimidothiazines indicates a promising specific antitumor agent against Hep-G2 cells with IC(50)<20 mu M

引用

页码：301 / 309

页数：9

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