Design, Synthesis, Antitumor and Antimicrobial Activity of Some Novel 6,7-Dimethoxyquinazoline Derivatives

Kassab, Asmaa E.; Gedawy, Ehab M.; Mahmoud, Zeinab; Khattab, Rania Abdelmonem

doi:10.3987/com-15-13329

Cited by 10 publications

(9 citation statements)

References 32 publications

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“…Compound is a hydrazone derivative attached to ciprofloxacin. The ciprofloxacin derivative bearing hydrazone moiety at 7-position 59a and 59b [94] showed significant in vitro antitumor activities with IC50 values 0.75 µM and 0.72 µM against UO-31 cancer cell line, respectively. Similarly, compound 59b displayed IC50 of 1.02 and 0.75 µM against NCI-H226 and IGROV1 cancer cell line, respectively.…”

Section: Modifications Of Fluoroquinolones At 7positionmentioning

confidence: 99%

Recent Strategies in Design of Antitumor and Antibacterial Fluoroquinolones

Samir

Ramadan

Hamed

et al. 2021

Journal of advanced Biomedical and Pharmaceutical Sciences

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Fluoroquinolones are known widely used synthetic antibacterial agents. Generally, there were some obstacles associated with their therapeutic use. Moreover, many research studies all over the world proved the variable biological effects of fluoroquinolones such as antituberculosis, anticancer, or even antiviral activities. The current review is focused on modifications that occurred in the fluoroquinolone scaffold for their repositioning from antibacterial into anticancer agents especially modifications at C-7 or at the carboxylic C-3 groups. In addition, it includes the recent research studies carried out to improve the potency, spectrum of activity, or pharmacokinetics of antibacterial fluoroquinolones. Hence, this review may be useful for researchers in the design and synthesis of new fluoroquinolones with improved biological activities.

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Section: Modifications Of Fluoroquinolones At 7positionmentioning

confidence: 99%

Recent Strategies in Design of Antitumor and Antibacterial Fluoroquinolones

Samir

Ramadan

Hamed

et al. 2021

Journal of advanced Biomedical and Pharmaceutical Sciences

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“…During apoptosis, mitochondria will undergo many changes, [ 20–22 ] including varying alterations in the mitochondrial membrane potential and the expression levels of many proteins such as caspases. [ 23,24 ] Many anticancer drugs act through the mitochondrial pathway. Also, the construction of QD fluorescence probes targeting mitochondria may guide the construction of QD nanodrug delivery systems.…”

Section: Introductionmentioning

confidence: 99%

Development of a Mitochondrially Targeted Probe Based on Polyethyleneimine‐(3‐carboxypropyl) Triphenylphosphine‐Modified Quantum Dots for Fluorescence Imaging

Zhang

Ren

Qiao

et al. 2020

Advanced Photonics Research

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Quantum dots (QDs) are semiconductor particles of a few nanometers in size that have unique optical and electronic properties. These properties include stable high‐intensity fluorescence and strong resistance to light bleaching, making them attractive as imaging agents. Mitochondria play many extremely important roles in cells. During apoptosis, several characteristics of mitochondria change that are exploited using fluorescent imaging probing including QDs. Herein, a mitochondria‐targetable fluorescence probe (CdSe/ZnS@PEI‐TPP) based on QDs is developed by covalently binding low‐molecular‐weight polyethyleneimine (PEI)‐modified CdSe/ZnS QDs with the small molecule (3‐carboxypropyl) triphenylphosphine (TPP). CdSe/ZnS@PEI‐TPP QDs have excellent optical emission properties. The ultraviolet and visible spectrophotometry (UV–vis) and fluorescence spectra of QDs show that TPP is successfully integrated into the QD structure. Cell proliferation measurements from 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide assays demonstrate that the modified QDs are less cytotoxic. The modified QDs show high fluorescence in cancer cells in vitro. These data demonstrate that CdSe/ZnS@PEI‐TPP QDs successfully target mitochondria and are used as fluorescence imaging probes.

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“…The pharmacological fight against cancer has made significant progress in the last twenty years. [4,5] Many papers have reported that pyrimidine derivatives showed impressive anticancer activity [6][7][8][9] and several members of this class have earned valued places in chemotherapy as effective agents, like 5-fluorouracil, tegafur, carmofur and fluoroadenosine. [1] Although many chemotherapeutic agents have been developed to treat different kinds of cancer effectively, some side effects could happen simultaneously.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antitumor Activity Evaluation of Pyrimidine Analogues Bearing Urea Moiety

Shao

Zhang

et al. 2014

Chin. J. Chem.

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A series of 4-anilino-6-phenylpyrimidines containing urea moiety were synthesized and the structures of all products were confirmed by 1 H NMR, 13 C NMR and HRMS. The antiproliferative activities of these compounds were evaluated against three human tumor cell lines (MGC-803, MCF-7 and EC-109) by applying the MTT assay method. compounds 4a, 4b and 6a showed the most effective activity, among which, 6a was more cytotoxic than 5-fluorouracil against all tested human cancer cell lines with IC 50 values ranging from 1.80 to 2.72 μmol•L -1 .

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Design, Synthesis, Antitumor and Antimicrobial Activity of Some Novel 6,7-Dimethoxyquinazoline Derivatives

Cited by 10 publications

References 32 publications

Recent Strategies in Design of Antitumor and Antibacterial Fluoroquinolones

Recent Strategies in Design of Antitumor and Antibacterial Fluoroquinolones

Development of a Mitochondrially Targeted Probe Based on Polyethyleneimine‐(3‐carboxypropyl) Triphenylphosphine‐Modified Quantum Dots for Fluorescence Imaging

Synthesis and Antitumor Activity Evaluation of Pyrimidine Analogues Bearing Urea Moiety

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