Design, synthesis and evaluation of acetylcholine-antitumor lipids hybrids lead to identification of a potential anticancer agent disrupting CDK4/6-Rb pathway in lung cancer DOI Creative Commons
Ahmed H.E. Hassan,

Eun Seo Bae,

Youngdo Jeong

et al.

RSC Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 1, 2025

Hybridization of acetylcholine with antitumor lipids (ATLs) was explored to achieve novel potential anticancer agents.

Language: Английский

Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective DOI Creative Commons
Adarsh Kumar, Ankit Kumar Singh, Harshwardhan Singh

et al.

Pharmaceuticals, Journal Year: 2023, Volume and Issue: 16(2), P. 299 - 299

Published: Feb. 14, 2023

Cancer is one of the major healthcare challenges across globe. Several anticancer drugs are available on market but they either lack specificity or have poor safety, severe side effects, and suffer from resistance. So, there a dire need to develop safer target-specific drugs. More than 85% all physiologically active pharmaceuticals heterocycles contain at least heteroatom. Nitrogen constituting most common heterocyclic framework. In this study, we compiled FDA approved with nitrogen atoms their pharmacological properties. Moreover, reported containing heterocycles, including pyrimidine, quinolone, carbazole, pyridine, imidazole, benzimidazole, triazole, β-lactam, indole, pyrazole, quinazoline, quinoxaline, isatin, pyrrolo-benzodiazepines, pyrido[2,3-d]pyrimidines, which used in treatment different types cancer, concurrently covering biochemical mechanisms action cellular targets.

Language: Английский

Citations

144

Potentials and future perspectives of multi-target drugs in cancer treatment: the next generation anti-cancer agents DOI Creative Commons
Ali Doostmohammadi,

Hossein Jooya,

Kimia Ghorbanian

et al.

Cell Communication and Signaling, Journal Year: 2024, Volume and Issue: 22(1)

Published: April 15, 2024

Abstract Cancer is a major public health problem worldwide with more than an estimated 19.3 million new cases in 2020. The occurrence rises dramatically age, and the overall risk accumulation combined tendency for cellular repair mechanisms to be less effective older individuals. Conventional cancer treatments, such as radiotherapy, surgery, chemotherapy, have been used decades combat cancer. However, emergence of novel fields research has led exploration innovative treatment approaches focused on immunotherapy, epigenetic therapy, targeted multi-omics, also multi-target therapy. hypothesis was based that drugs designed act against individual targets cannot usually battle multigenic diseases like Multi-target therapies, either combination or sequential order, recommended acquired intrinsic resistance anti-cancer treatments. Several studies multi-targeting treatments due their advantages include; overcoming clonal heterogeneity, lower multi-drug (MDR), decreased drug toxicity, thereby side effects. In this study, we'll discuss about drugs, benefits improving recent advances field multi-targeted drugs. Also, we will study performed clinical trials using therapeutic agents treatment.

Language: Английский

Citations

36

1,2,3-triazole and chiral Schiff base hybrids as potential anticancer agents: DFT, molecular docking and ADME studies DOI Creative Commons
Yonas Belay, Alfred Muller,

Fanikie S. Mokoena

et al.

Scientific Reports, Journal Year: 2024, Volume and Issue: 14(1)

Published: March 23, 2024

Abstract A series of novel 1,2,3-triazole and chiral Schiff base hybrids 2 – 6 were synthesized by condensation reaction from pre-prepared parent component the (1,2,3-triazole 1) primary amines their chemical structure confirmed using NMR FTIR spectroscopies, CHN elemental analysis. Compounds 1 evaluated for anticancer activity against two cancer PC3 (prostate) A375 (skin) MRC-5 (healthy) cell lines Almar Blue assay method. The compounds exhibited significant cytotoxicity tested lines. Among 3 showed very good inhibition low toxicity healthy All high binding affinity Androgen receptor modulators (PDB ID: 5t8e) Human MIA 1i1j) inhibitors compared to reference drug (cisplatin). Structure relationships (SARs) is in agreement with DFT molecular docking studies. desirable physicochemical properties likeness.

Language: Английский

Citations

23

Ferrocene-Based Drugs, Delivery Nanomaterials and Fenton Mechanism: State of the Art, Recent Developments and Prospects DOI Creative Commons
Cátia Ornelas, Didier Astruc

Pharmaceutics, Journal Year: 2023, Volume and Issue: 15(8), P. 2044 - 2044

Published: July 29, 2023

Ferrocene has been the most used organometallic moiety introduced in organic and bioinorganic drugs to cure cancers various other diseases. Following several pioneering studies, two real breakthroughs occurred 1996 1997. In 1996, Jaouen et al. reported ferrocifens, ferrocene analogs of tamoxifen, chemotherapeutic for hormone-dependent breast cancer. Several ferrocifens are now preclinical evaluation. Independently, 1997, ferroquine, an analog antimalarial drug chloroquine upon introduction a ferrocenyl substituent carbon chain, was by Biot-Brocard group found be active against both chloroquine-sensitive chloroquine-resistant strains Plasmodium falciparum. Ferroquine, combination with artefenomel, completed phase IIb clinical evaluation 2019. More than 1000 studies have published on ferrocenyl-containing pharmacophores infectious diseases, including parasitic, bacterial, fungal, viral infections, but relationship between structure biological activity scarcely demonstrated, unlike ferroquines. majority ferrocene-containing drugs, however, production reactive oxygen species (ROS), particular OH. radical, produced Fenton catalysis, plays key role is scrutinized this mini-review, together supramolecular approach utilizing delivery nanosystems, such as micelles, metal–organic frameworks (MOFs), polymers, dendrimers.

Language: Английский

Citations

40

Current scenario of pyrazole hybrids with in vivo therapeutic potential against cancers DOI

Zhi Xu,

Yafei Zhuang,

Qingtai Chen

et al.

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 257, P. 115495 - 115495

Published: May 16, 2023

Language: Английский

Citations

27

Design and synthesis of some novel hybrid molecules based on 4-thiazolidinone bearing pyridine-pyrazole scaffolds: molecular docking and molecular dynamics simulations of its major constituent onto DNA gyrase inhibition DOI
Nisheeth C. Desai, Dharmpalsinh J. Jadeja, Aratiba M. Jethawa

et al.

Molecular Diversity, Journal Year: 2023, Volume and Issue: 28(2), P. 693 - 709

Published: Feb. 8, 2023

Language: Английский

Citations

23

Carvacrol and Thymol Hybrids: Potential Anticancer and Antibacterial Therapeutics DOI Creative Commons
Sijongesonke Peter, Namhla Sotondoshe, Blessing A. Aderibigbe

et al.

Molecules, Journal Year: 2024, Volume and Issue: 29(10), P. 2277 - 2277

Published: May 12, 2024

Cancer is ranked among lethal diseases globally, and the increasing number of cancer cases deaths results from limited access to effective therapeutics. The use plant-based medicine has been gaining interest several researchers. Carvacrol its isomeric compound, thymol, are extracts that possess biological activities, such as antimalarial, anticancer, antifungal, antibacterial. However, their efficacy compromised by poor bioavailability. Thus, medicinal scientists have explored synthesis hybrid compounds containing pharmacophores enhance therapeutic improve Hence, this review a comprehensive report on carvacrol isomer, with potent anticancer antibacterial agents reported between 2020 2024. Furthermore, structural activity relationship (SAR) recommended future strategies further effects will be discussed.

Language: Английский

Citations

9

Development of novel triconjugates fusing melatonin/isatin/N-acylhydrazone targeting colorectal cancer: design, synthesis, biological, and in silico ADME/Tox profiling DOI
Sergio Gutiérrez, Wilson Cardona‐G, Angie Herrera‐Ramírez

et al.

Medicinal Chemistry Research, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 7, 2025

Language: Английский

Citations

1

Synthesis, Molecular Docking Study, and Cytotoxicity Evaluation of Some Novel 1,3,4-Thiadiazole as Well as 1,3-Thiazole Derivatives Bearing a Pyridine Moiety DOI Creative Commons
Amr S. Abouzied, Jehan Y. Al‐Humaidi, Abdulrahman S. Bazaid

et al.

Molecules, Journal Year: 2022, Volume and Issue: 27(19), P. 6368 - 6368

Published: Sept. 27, 2022

Pyridine, 1,3,4-thiadiazole, and 1,3-thiazole derivatives have various biological activities, such as antimicrobial, analgesic, anticonvulsant, antitubercular, well other anticipated properties, including anticancer activity. The starting 1-(3-cyano-4,6-dimethyl-2-oxopyridin-1(2H)-yl)-3-phenylthiourea (2) was prepared reacted with hydrazonoyl halides 3a-h, α-haloketones 5a-d, 3-chloropentane-2,4-dione 7a ethyl 2-chloro-3-oxobutanoate 7b, which afforded the 3-aryl-5-substituted 1,3,4-thiadiazoles 4a-h, 3-phenyl-4-arylthiazoles 6a-d 4-methyl-3- phenyl-5-substituted thiazoles 8a,b, respectively. structures of synthesized products were confirmed by spectral data. All compounds also showed remarkable activity against cell line human colon carcinoma (HTC-116) hepatocellular (HepG-2) compared Harmine a reference under in vitro condition. 1,3,4-Thiadiazole 4h found to be most promising an excellent performer both cancer lines (IC50 = 2.03 ± 0.72 2.17 0.83 µM, respectively), better than drug 2.40 0.12 2.54 0.82 respectively). In order check binding modes above thiadiazole derivatives, molecular docking studies performed that established site EGFR TK.

Language: Английский

Citations

32

Selenium-Containing Agents Acting on Cancer—A New Hope? DOI Creative Commons
Sabrina Garbo, Silvia Di Giacomo, Dorota Łażewska

et al.

Pharmaceutics, Journal Year: 2022, Volume and Issue: 15(1), P. 104 - 104

Published: Dec. 28, 2022

Selenium-containing agents are more and considered as an innovative potential treatment option for cancer. Light is shed not only on the considerable advancements made in understanding complex biology chemistry related to selenium-containing small molecules but also Se-nanoparticles. Numerous Se-containing have been widely investigated recent years cancer therapy relation tumour development dissemination, drug delivery, multidrug resistance (MDR) immune system-related (anti)cancer effects. Despite numerous efforts, Se-agents apart from selenocysteine selenomethionine yet reached clinical trials therapy. The purpose of this review provide a concise critical overview current state art highly potent target-specific agents.

Language: Английский

Citations

31