Synthesis, Biological Evaluation and Stability Studies of Some Novel Aza-Acridine Aminoderivatives

被引：6

作者：

Karelou, Maria ^{[1
]}

Kourafalos, Vasileios ^{[1
]}

Tragomalou, Athanasia P. ^{[2
,4
]}

Marakos, Panagiotis ^{[1
]}

Pouli, Nicole ^{[1
]}

Tsitsilonis, Ourania E. ^{[2
]}

Gikas, Evangelos ^{[3
]}

Kostakis, Ioannis K. ^{[1
]}

机构：

[1] Natl & Kapodistrian Univ Athens, Div Pharmaceut Chem, Dept Pharm, Athens 15771, Greece

[2] Natl & Kapodistrian Univ Athens, Dept Biol, Sect Anim & Human Physiol, Athens 15771, Greece

[3] Natl & Kapodistrian Univ Athens, Dept Chem, Analyt Chem Lab, Athens 15771, Greece

[4] Natl & Kapodistrian Univ Athens, Aghia Sophia Childrens Hosp, Sch Med, Div Endocrinol Metab & Diabet,Dept Pediat 1, Athens 15771, Greece

来源：

MOLECULES | 2020年 / 25卷 / 19期

关键词：

acridines; cancer; drug discovery; stability; computational chemistry; mass spectrometry; OVERCOME MULTIDRUG-RESISTANCE; ANTIPROLIFERATIVE ACTIVITY; ACRONYCINE DERIVATIVES; DESIGN; TAUTOMERISM; XANTHENONES; MECHANISM;

D O I：

10.3390/molecules25194584

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：

Several new amino-substituted aza-acridine derivatives bearing a basic side chain have been designed and synthesized. The antiproliferative activity of the target compounds has been evaluated against three cancer cell lines-namely HCT-116 (colorectal), the uterine sarcoma MES-SA, and its doxorubicin-resistant variant MES-SA/Dx5. A limited number of the new acridines showed marginal cytotoxicity against the tested cell lines; nevertheless, these analogues possessed a similar substitution pattern. The moderate biological activity of these derivatives was attributed to their instability in aqueous media, which has been studied by mass spectrometry and computational chemistry experiments at the density functional level of theory (DFT).

引用

页数：16

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