Synthesis and in vitro evaluation of the anticancer activity of novel fluorinated thiazolo[4,5-d]pyrimidines

被引:55
作者
Fahmy, HTY
Rostom, SAF
Saudi, MN
Zjawiony, JK
Robins, DJ
机构
[1] Univ Mississippi, Sch Pharm, Dept Pharmacognosy, University, MS 38677 USA
[2] Univ Alexandria, Fac Pharm, Dept Pharmaceut Chem, Alexandria, Egypt
[3] Univ Glasgow, Dept Chem, Glasgow G12 8QQ, Lanark, Scotland
关键词
thaizole; fluorinated; thiazolo[4,5-d]pyrimidines; anticancer activity;
D O I
10.1002/ardp.200300734
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of several thiazolo[4,5-d]pyrimidines containing a fluorophenyl moiety substituted at different positions and through different bridges is described. Twenty new compounds were prepared and evaluated for their anticancer activity using the USA-NCl in-vitro screening program. Three compounds were found active and their anticancer activity against 60 human tumor cell lines are described in detail.
引用
收藏
页码:216 / 225
页数:10
相关论文
共 25 条
[1]   FLUORINATED MEDICINALS [J].
ABOULENEIN, HY .
TOXICOLOGICAL AND ENVIRONMENTAL CHEMISTRY, 1991, 29 (04) :235-249
[2]   ANTICANCER SPECIFICITY OF SOME ELLIPTICINIUM SALTS AGAINST HUMAN BRAIN-TUMORS IN-VITRO [J].
ACTON, EM ;
NARAYANAN, VL ;
RISBOOD, PA ;
SHOEMAKER, RH ;
VISTICA, DT ;
BOYD, MR .
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (14) :2185-2189
[3]   POTENTIAL ANTI-MICROBIALS .1. SYNTHESIS AND STRUCTURE-ACTIVITY STUDIES OF SOME NEW THIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES [J].
BADAWEY, ESAM ;
RIDA, SM ;
HAZZA, AA ;
FAHMY, HTY ;
GOHAR, YM .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1993, 28 (02) :91-96
[4]   POTENTIAL ANTI-MICROBIALS .2. SYNTHESIS AND INVITRO ANTIMICROBIAL EVALUATION OF SOME THIAZOLO[4,5-D]PYRIMIDINES [J].
BADAWEY, ESAM ;
RIDA, SM ;
HAZZA, AA ;
FAHMY, HTY ;
GOHAR, YM .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1993, 28 (02) :97-101
[5]  
BECK J, 1999, Patent No. 9951608
[6]   Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists [J].
Beck, JP ;
Curry, MA ;
Chorvat, RJ ;
Fitzgerald, LW ;
Gilligan, PJ ;
Zaczek, R ;
Trainor, GL .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (08) :1185-1188
[7]  
BERGER A, 1971, Patent No. 2038922
[8]   SYNTHESIS OF CERTAIN N-ALKYL AND C-ALKYL PURINE ANALOGS [J].
BHATTACHARYA, BK ;
RAO, TS ;
LEWIS, AF ;
REVANKAR, GR ;
SANGHVI, YS ;
ROBINS, RK .
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1993, 30 (05) :1341-1349
[9]   SOME PRACTICAL CONSIDERATIONS AND APPLICATIONS OF THE NATIONAL-CANCER-INSTITUTE IN-VITRO ANTICANCER DRUG DISCOVERY SCREEN [J].
BOYD, MR ;
PAULI, KD .
DRUG DEVELOPMENT RESEARCH, 1995, 34 (02) :91-109
[10]   ON THE CHEMISTRY OF 4-AMINOTHIAZOLINE-2-THIONES [J].
GEWALD, K ;
HAIN, U ;
HARTUNG, P .
MONATSHEFTE FUR CHEMIE, 1981, 112 (12) :1393-1404