DHFR inhibitors: reading the past for discovering novel anticancer agents

MV Raimondi, O Randazzo, M La Franca, G Barone… - Molecules, 2019 - mdpi.com
Dihydrofolate reductase inhibitors are an important class of drugs, as evidenced by their use
as antibacterial, antimalarial, antifungal, and anticancer agents. Progress in understanding …

Trimethoprim and other nonclassical antifolates an excellent template for searching modifications of dihydrofolate reductase enzyme inhibitors

A Wróbel, K Arciszewska, D Maliszewski… - The Journal of …, 2020 - nature.com
The development of new mechanisms of resistance among pathogens, the occurrence and
transmission of genes responsible for antibiotic insensitivity, as well as cancer diseases …

Dihydrofolate reductase inhibitors for use as antimicrobial agents

J He, W Qiao, Q An, T Yang, Y Luo - European journal of medicinal …, 2020 - Elsevier
Drug-resistant bacteria pose an increasingly serious threat to mankind all over the world.
However, the currently available clinical treatments do not meet the urgent demand …

Exploration and Biological Evaluation of 1,3-Diamino-7H-pyrrol[3,2-f]quinazoline Derivatives as Dihydrofolate Reductase Inhibitors

Z Zhu, C Chen, J Zhang, F Lai, J Feng… - Journal of Medicinal …, 2023 - ACS Publications
Dihydrofolate reductase (DHFR), a core enzyme of folate metabolism, plays a crucial role in
the biosynthesis of purines and thymidylate for cell proliferation and growth in both …

Dihydrofolate reductase inhibitors: Patent landscape and phases of clinical development (2001–2021)

K Bhagat, N Kumar, H Kaur Gulati… - Expert Opinion on …, 2022 - Taylor & Francis
Introduction Dihydrofolate reductase (DHFR) plays an important role in the biosynthesis of
amino acid and folic acid. It participates by reducing dihydrofolate to tetrahydrofolate, in the …

Synthesis, antimicrobial and α-glucosidase inhibition of new benzimidazole-1, 2, 3-triazole-indoline derivatives: a combined experimental and computational venture

L Deswal, V Verma, D Kumar, Y Deswal, A Kumar… - Chemical Papers, 2022 - Springer
In the current research work, a new series of benzimidazole-1, 2, 3-triazole-indoline
derivatives (5a–r) were designed and synthesized by employing click reaction between …

Cinnamomum zeylanicum Extract and its Bioactive Component Cinnamaldehyde Show Anti-Tumor Effects via Inhibition of Multiple Cellular Pathways

S Aggarwal, K Bhadana, B Singh, M Rawat… - Frontiers in …, 2022 - frontiersin.org
Cinnamomum zeylanicum is a tropical plant with traditional medicinal significance that
possesses antimicrobial, antifungal, anti-parasitic, and anti-tumor properties. Here, we have …

Design and Synthesis of a New Class of Pyridine-Based N-Sulfonamides Exhibiting Antiviral, Antimicrobial, and Enzyme Inhibition Characteristics

RA Azzam, RE Elsayed, GH Elgemeie - ACS omega, 2020 - ACS Publications
A new strategy for designing and assembling a novel class of functionalized pyridine-based
benzothiazole and benzimidazole incorporating sulfonamide moieties was developed. The …

Potential bacterial biofilm, MRSA, and DHFR inhibitors based on new morpholine-linked chromene-thiazole hybrids: One-pot synthesis and in silico study

SMH Sanad, AEM Mekky, TT El-Idreesy - Journal of Molecular Structure, 2022 - Elsevier
We report herein the utility of the morpholine-linked benzaldehyde as a key building block in
the preparation of two series of new chromene-thiazoles with potential bioactivities. In this …

An insight into synthetic strategies and recent developments of dihydrofolate reductase inhibitors

P Chawla, G Teli, RK Gill, RK Narang - ChemistrySelect, 2021 - Wiley Online Library
The dihydrofolate reductase (DHFR) is a significant target in cancer, microbial infection,
fungal infection, malaria, leishmaniasis, and tuberculosis, among other diseases. The DHFR …