Development of heterocyclic-based anticancer agents: A comprehensive review

Heterocyclic Communications, Journal Year: 2025, Volume and Issue: 31(1)

Published: Jan. 1, 2025

Abstract This review article summarizes the role of heterocyclic compounds as anticancer drugs used against various human cancers, including doxorubicin, cisplatin, paclitaxel, and resveratrol, which are among most effective therapeutic agents. Chemotherapy, a treatment modality, exerts its effects on tumor cell DNA often involves use low-molecular-weight medicines to selectively target destroy cancer cells. However, systemic chemotherapy is associated with several side effects, such nausea, vomiting, myelosuppression, cardiotoxicity. Cancer remains one prevalent lethal diseases, characterized by uncontrolled division abnormal growth driven multiple genetic mutations. The etiopathogenesis complex, but significant advancements have been made in treatment, particularly discovery drugs, cytotoxic chemotherapy, hormonal agents, targeted therapies. Anticancer widely employed for breast, cervical, uterine, kidney cancers. These classified into categories, alkylating antimetabolites, antibiotics, topoisomerase inhibitors. Among these, numerous shown promising properties. goal this compile information highlighting their positive targets chemoprevention.

Language: Английский

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Physicochemical Characterization, Metabolite Profiling, and Preclinical Pharmacokinetic Assessment of a Sulfonamide‐Based Pyruvate Kinase M2 Activator for Anticancer Lead Identification

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(16)

Published: April 1, 2025

Abstract This study investigates the pharmacokinetic, physicochemical, and metabolite properties of 9b , a novel imidazopyrimidine‐based sulfonamide previously shown to be effective against A549 lung adenocarcinoma cell line. Aiming evaluate its ADME (absorption, distribution, metabolism, excretion) characteristics for drug development, found that possesses favorable physicochemical properties, including pKa 12.35, LogP 2.89, LogD 0.98. Stability tests demonstrated remains stable in human plasma liver microsomes up 1 h, with moderate protein binding (46%). Metabolite profiling using LC/Q‐TOF MS revealed three major metabolites ( M1 M2 M3 ), whereas vivo pharmacokinetic analysis via LC/QQQ‐MS indicated optimal parameters, C max T AUC, half‐life (t 1/2 ) consistent balanced profile. These results highlight ’s promising stability, binding, metabolic profile, positioning it as strong candidate further development an anticancer drug. Given impressive efficacy cancer lines, shows significant potential advancing treatment.

Language: Английский

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Synthesis, characterization, and biological activities investigation of tri-armed structure of (7-bromo-5-chloro- 2,3-dihydrophthalazine-1,4-dione) based on benzene ring

Journal of Chemical Research, Journal Year: 2024, Volume and Issue: 48(6)

Published: Nov. 1, 2024

Due to the importance of heterocyclic rings in drug design, we synthesized a novel multicyclic compound, designated as (2,2′,2ʺ-(benzene-1,3,5-tricarbonyl) tris(6-bromo-4-chloroisobenzofuran-1,3-dione) (compound D), under mild conditions and within an acidic medium. The synthesis this valuable compound commenced with preparation benzene-1,3,5-tricarbohydrazide from benzene-1,3,5-tricarboxylic acid hydrazine hydrate. This transitional was subsequently interacted 6-bromo-4-chloroisobenzofuran-1,3-dione yield target D. compounds were purified, their structures elucidated through advanced spectroscopic techniques, including Fourier-transform infrared (FTIR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy ( 1 H NMR, 13 C NMR). Gram-negative Escherichia coli) gram-positive Staphylococcus aureus) bacteria used evaluate antibacterial activity produced compound. bioactivity new compared that conventional antibiotics, such ampicillin streptomycin. Interestingly, D exhibited according reference drugs. Furthermore, molecular docking studies have shown many connections amino residues active sites, thus these results possibility inspire further investigation field compounds.

Language: Английский

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Anti-Breast Cancer Potential of New Indole Derivatives: Synthesis, In-Silico Study, and Cytotoxicity Evaluation on MCF-7 Cells

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: unknown, P. 141176 - 141176

Published: Dec. 1, 2024

Language: Английский

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