Synthesis of 5-and 6-N-heterocyclic Methylenebisphosphonate Derivatives and Evaluation of their Cytogenetic Activity in Normal Human Lymphocyte Cultures

被引：20
作者：
Abdou, Wafaa M. [1 ]
Kamel, Azza A. [1 ]
Khidre, Rizk E. [1 ]
Geronikaki, Athina [2 ]
Ekonomopoulou, Maria T. [3 ]
机构：
[1] Natl Res Ctr, Chem Ind Div, Cairo, Egypt
[2] Aristotle Univ Thessaloniki, Sch Pharm, Dept Pharmaceut Chem, GR-54006 Thessaloniki, Greece
[3] Aristotle Univ Thessaloniki, Lab Gen Biol & Genet, Sch Med, GR-54006 Thessaloniki, Greece
来源：
CHEMICAL BIOLOGY & DRUG DESIGN | 2012年 / 79卷 / 05期
关键词：
bisphosphonates; cytogenetic activity; cytotoxic; cytostatic properties; insertion reaction; oxazinones; Schiff bases; BIOLOGICAL-ACTIVITY SPECTRA; CLASTOGENIC ACTIVITIES; CANCER; PREDICTION; REACTIVITY; INHIBITORS; EFFICIENT; DESIGN; ACIDS; SETS;
D O I：
10.1111/j.1747-0285.2012.01327.x
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Methods for the preparation of various aminomethylene bisphosphonates were developed. The required bisphosphonates were obtained by applying tetraethyl methylenebisphosphonate reagent to different types of oxazinones and the relevant Schiff base derivatives. Based on the prediction results (Pass program), we further estimated the sister chromatid exchange frequency and proliferation rate index values of human lymphocyte cultures after the administration of four newly synthesized bisphosphonates in order to evaluate their cytotoxic/cytostatic and possible antineoplastic potency. The results showed that all four bisphosphonates cause a dose-dependent increase in sister chromatid exchange frequency, followed by a decrease in proliferation rate index in both experiments compared to the control.
引用
收藏
页码：719 / 730
页数：12
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