Camptothecin structure simplification elaborated new imidazo[2,1-b]quinazoline derivative as a human topoisomerase I inhibitor with efficacy against bone cancer cells and colon adenocarcinoma

Khodair, Ahmed I.; El-Hallouty, Salwa M.; Cagle-White, Brittnee; Abdel Aziz, May H.; Hanafy, Mahmoud Kh.; Mowafy, Samar; Hamdy, Nadia M.; Kassab, Shaymaa E.

doi:10.1016/j.ejmech.2023.116049

Cited by 4 publications

(1 citation statement)

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“…Inhibition of these enzymes leads to blocking and disruption of the DNA structure [ 27 ]. Two types of topoisomerases are identified, I and II, based on whether they work on single or double strands [ 28 ]. The regular cell cycle utilizes these enzymes for performing essential processes like transcription, replication, and recombination during DNA synthesis.…”

Section: Reviewmentioning

confidence: 99%

Quinazoline Derivatives as Targeted Chemotherapeutic Agents

Zayed

2024

Cureus

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Most of the current chemotherapeutic medications are extremely toxic, exhibit little selectivity, and contribute to the emergence of treatment resistance. Consequently, the discovery of targeted chemotherapy drugs with high selectivity and low side effects is necessary for cancer treatment. The quinazoline system has a broad range and a long history of biological activities. Numerous quinazoline derivatives have been used to treat different types of cancer by working on various molecular targets. This review presents various chemical information, including molecular structure, design, and biological activity of some reported quinazolines that function by inhibiting four types of important molecular targets: dihydrofolate reductase, breast cancer resistant protein, poly-(ADP-ribose)-polymerase, and tubulin polymerization.

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Section: Reviewmentioning

confidence: 99%

Quinazoline Derivatives as Targeted Chemotherapeutic Agents

Zayed

2024

Cureus

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Design, Synthesis, Antibacterial, and Antifungal Evaluation of a New Series of Quinazoline – Thiazole and/or Quinazoline – Triazole Hybrids as Bioactive Heterocycles

El‐Shahat,

Tawfek,

El‐Sofany

2024

Chemistry & Biodiversity

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Herein, a one‐pot reaction between cyclohexanone, thiourea, and 2,5‐dimethoxybenzaldehyde allowed to prepare hexahydroquinazoline‐2(1H)‐thione 4 firstly, which dollowed by reacting with hydrazine hydrate to produce the corresponding 2‐hydrazinylhexahydroquinazoline 6. Interesting analogs of thiazolo[3,2‐a]quinazoline 7‐13 where obtained when hexahydroquinazoline‐2(1H)‐thione 4 reacted with 1,2‐dibromoethane, chloroacetyl chloride, bromoacetic acid, bromoacetic acid/4‐chlorobenzaldehyde, 2‐bromopropionic acid, ethyl bromocyanoacetate, and/or bromomalononitrile; respectively. While triazolo[4,3‐a] quinazoline 14‐16 were created when 2‐hydrazinylhexahydroquinazoline 6 reacted with triethyl orthoformate, acetic anhydride, and carbon disulfide respectively. Additionally, the new analogs were examined for their antibacterial and antifungal properties against Escherichia coli, Staphylococcus aureus, and Candida albicans. It was discovered that triazolo[4,3‐a] quinazoline analogs 14‐16 have superior bacterial and fungal activity when compared to the corresponding conventional doses of Streptomycin and Griseofulvin. Towards Candida albicans; compounds 14, 15, and 16 increase activity with 1.14%, 1.15%, and 1.21%, respectively more than griseofulvin.While, for Staphylococcus aureus; compounds 14, 15, and 16 increase activity with 1.5%, 1.5%, and 1.7%, respectively more than streptomycin. Morever, for Escherichia coli; compounds 14, 15, and 16 increase activity with 1.19%, 1.21%, and 1.22%, respectively more than streptomycin. Finally, structure activity relationships show that quinazoline derivatives exhibit higher activity when fused to pyrazole ring 14–16 as compared when fused thiophene ring 7–13.

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