3,7-bis-benzylidene hydrazide ciprofloxacin derivatives as promising antiproliferative dual TOP I &amp; TOP II isomerases inhibitors

Samir, M.; Ramadan, Mohamed; Abdelrahman, Mostafa H.; Abdelbaset, Mahmoud S.; Abourehab, Mohammed A. S.; Abdel‐Aziz, Mohamed; Abuo‐Rahma, Gamal El‐Din A.

doi:10.1016/j.bioorg.2021.104698

Cited by 12 publications

(7 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In addition to, compounds 98a, 98b, and 98c exhibited promising dual Topo I and II inhibitory activities with IC50, (16.6, 12.1 and 15.1 µM for Topo Iα) and (120.9. 97.3 and 86.5 pg/ml for Topo IIB) comparable to Camptothecin IC5o, 10.5 µM, and Etoposide IC50, 90.6 pg/ml, respectively [129].…”

Section: Modifications Of Fluoroquinolones At 3 and 7positionmentioning

confidence: 77%

“…Compounds 98a-c are 3,7-bis-benzylidenes hybrids of ciprofloxacin. These hybrids exhibited potent antiproliferative activity comparable to Doxorubicin against leukemia cancer cell line HL-60 (TB) colon cancer cell line HCT-116, breast cancer cell line MCF7, and induced apoptosis at G2/M phase, as well as exhibited promising dual Topo Iα and Topo IIB inhibition activities comparable to reference drugs Camptothecin and Etoposide [129]. New strategies for developing new antibacterial fluoroquinolones analogs are necessary to improve the antibacterial activities of fluoroquinolones against different species of organism, including Gram-positive, Gram-negative, aerobic, and anaerobic bacteria.…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Recent Strategies in Design of Antitumor and Antibacterial Fluoroquinolones

Samir

Ramadan

Hamed

et al. 2021

Journal of advanced Biomedical and Pharmaceutical Sciences

Self Cite

View full text Add to dashboard Cite

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.

show abstract

Section: Modifications Of Fluoroquinolones At 3 and 7positionmentioning

confidence: 77%

Section: Discussionmentioning

confidence: 99%

Recent Strategies in Design of Antitumor and Antibacterial Fluoroquinolones

Samir

Ramadan

Hamed

et al. 2021

Journal of advanced Biomedical and Pharmaceutical Sciences

Self Cite

View full text Add to dashboard Cite

show abstract

“…In 2021, a new series of 3,7‐bis‐benzylidenes of CP was designed and synthesized, according to Samir et al [ 89 ] Most of the target compounds demonstrated good cytotoxic activity; however, the most potent compounds 32a and 32b (Figure 32) achieved strong broad‐spectrum antiproliferative activity with IC 50 values of 1.21, 0.87, 1.21, 0.41, 0.57 and 1.31 µM that was comparable to doxorubicin with IC 50 values 1.26, 1.79 and 0.63 µM against the leukemia cancer cell line HL‐60 (TB), colon cancer cell line HCT‐116, and breast cancer cell line MCF‐7, respectively. Additionally, the most potent derivative 32b , caused apoptosis at the G2/M phase.…”

Section: N‐acylhydrazones As Anticancer Agentsmentioning

confidence: 99%

“…A roughly twofold increase in efficacy was seen when a hydrogen bond donor group (6-aminopyridin-3-yl substituent) was added at position 4. [88] In 2021, a new series of 3,7-bis-benzylidenes of CP was designed and synthesized, according to Samir et al [89] Most of the target compounds demonstrated good cytotoxic activity; however, the most potent compounds 32a and 32b (Figure 32 In the same year, Kassab et al [90] reported the design and hydrazones were harmful to the common HEK-293 human embryonic kidney cell line. [91] A number of novel N-acylhydrazone derivatives with the benzothiazole and indole-based moiety were developed, synthesized, and tested for in vitro antiproliferative activity against the Hep G2 cancer cell line using a structure-based molecular hybridization method.…”

Section: N-acylhydrazones As Antiangiogenesis Agentsmentioning

confidence: 99%

Anticancer agents incorporating the N‐acylhydrazone scaffold: Progress from 2017 to present

Kassab

2023

Archiv der Pharmazie

View full text Add to dashboard Cite

The N-acylhydrazone motif has been shown to be particularly adaptable and promising in the area of medicinal chemistry and drug development, due to its significant biological and pharmacological characteristics. Moreover, N-acylhydrazones are appealing synthetic and biological tools because of their simple and straightforward synthesis. This scaffold has emerged as a fundamental building block for the synthesis of bioactive compounds.Particularly, the N-acylhydrazone scaffold served as a base for the synthesis of a number of potent anticancer agents acting via different mechanisms. An updated summary of the anticancer activity of N-acylhydrazone derivatives described in the literature (from 2017 to 2022) is provided in the current review. It discusses the structure-activity relationship (SAR) of N-acylhydrazone derivatives exhibiting anticancer potential, which could be helpful in designing and developing new derivatives as effective antiproliferative candidates in the future.

show abstract

“…Furthermore, the antiproliferative effect of synthesized analogues were tested versus the NCI‐60 cell panel, which comprises of melanoma, leukemia, lung, colon, ovarian, renal, and breast cancer cell lines. Compound 12c and 12b showed wide range of cytotoxic activities against leukemia cancer cell line HL‐60 (1.21 ± 0.02 μM & 0.41 ± 0.02), colon cancer cell line HCT‐116 (0.87 ± 0.04 μM and 0.57 ± 0.06), and breast cancer cell line MCF7 (1.21 ± 0.02 μM and 1.31 ± 0.04) respectively [ 75 ] (Figure 16).…”

Section: Nitrogen Containing Heterocycles As Inhibitors Of Topoisomer...mentioning

confidence: 99%

Nitrogen‐containing heterocycles as topoisomerase II inhibitors for targeting cancer: Recent updates

Sahu

Chaurasiya

Chawla

2022

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

Cancer is a broad word for a set of diseases that can begin in virtually any organ or tissue of the body and spread to other organs. In 2020, cancer was the largest cause of death worldwide, accounting for 10 million fatalities, or one in every six deaths. Nitrogen containing heterocyclic compounds are a massive research focus because it has a unique position and is a cherished source of a wide range of bioactive molecules in medicinal chemistry. Over 75% of the currently accessible market is covered by FDA-approved drugs containing nitrogen moieties. DNA topoisomerase II is a reassuring approach for novel anticancer heterocyclic medicines because it plays a crucial role in DNA metabolism, replication, recombination, and repair. Given the importance of topo II in chemotherapy, there is a pressing necessity to boost topo II or multitarget topo II inhibitors in order to combat drug resistance and minimize toxicity. Following the trend of researching the advancement of effective topo II inhibitors with minimal toxicity, the current review article consolidates a detailed account of nitrogen-containing heterocyclic compounds and categorizes them into different classes based on structural characterization, such

show abstract

3,7-bis-benzylidene hydrazide ciprofloxacin derivatives as promising antiproliferative dual TOP I & TOP II isomerases inhibitors

Cited by 12 publications

References 23 publications

Recent Strategies in Design of Antitumor and Antibacterial Fluoroquinolones

Recent Strategies in Design of Antitumor and Antibacterial Fluoroquinolones

Anticancer agents incorporating the N‐acylhydrazone scaffold: Progress from 2017 to present

Nitrogen‐containing heterocycles as topoisomerase II inhibitors for targeting cancer: Recent updates

Contact Info

Product

Resources

About