DNA and RNA synthesis: antifolates

IM Kompis, K Islam, RL Then - Chemical reviews, 2005 - ACS Publications
Tetrahydrofolate cofactors are essential for the synthesis of purines, certain amino acids,
and thymidine. Most bacteria and plants produce these folate cofactors by de novo …

Recent advances in classical and non-classical antifolates as antitumor and antiopportunistic infection agents: Part II

A Gangjee, HD Jain, S Kurup - Anti-Cancer Agents in Medicinal …, 2008 - ingentaconnect.com
Antifolates that inhibit the key enzymes thymidylate synthase (TS) and dihydrofolate
reductase (DHFR) have found clinical utility as antitumor and antiopportunistic agents …

Molecular fingerprint-based artificial neural networks QSAR for ligand biological activity predictions

KZ Myint, L Wang, Q Tong, XQ Xie - Molecular pharmaceutics, 2012 - ACS Publications
In this manuscript, we have reported a novel 2D fingerprint-based artificial neural network
QSAR (FANN-QSAR) method in order to effectively predict biological activities of structurally …

Pharmacophore Mapping of a Series of 2,4-Diamino-5-deazapteridine Inhibitors of Mycobacterium avium Complex Dihydrofolate Reductase

AK Debnath - Journal of medicinal chemistry, 2002 - ACS Publications
Pharmacophore hypotheses were developed for a series of 2, 4-diamino-5-deazapteridine
inhibitors of Mycobacterium avium complex (MAC) and human dihydrofolate reductase …

Discovery of new 1, 3, 5-triazine scaffolds with potent activity against Mycobacterium tuberculosis H37Rv

N Sunduru, L Gupta, V Chaturvedi, R Dwivedi… - European Journal of …, 2010 - Elsevier
A series of eighty one 2, 4, 6-trisubstituted-1, 3, 5-triazines were synthesized and evaluated
in vitro for the growth inhibition of Mycobacterium tuberculosis H37Rv. Fifteen compounds …

Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole

WT Ashton, RM Sisco, H Dong, KA Lyons, H He… - Bioorganic & medicinal …, 2005 - Elsevier
A series of β-aminoacylpiperidines bearing various fused five-membered heterocyclic rings
was synthesized as dipeptidyl peptidase IV inhibitors. Potent and relatively selective …

Synthesis and biological activity of N4-phenylsubstituted-6-(2, 4-dichloro phenylmethyl)-7H-pyrrolo [2, 3-d] pyrimidine-2, 4-diamines as vascular endothelial growth …

A Gangjee, S Kurup, MA Ihnat, JE Thorpe… - Bioorganic & medicinal …, 2010 - Elsevier
A series of eight N4-phenylsubstituted-6-(2, 4-dichlorophenylmethyl)-7H-pyrrolo [2, 3-d]
pyrimidine-2, 4-diamines 8–15 were synthesized as vascular endothelial growth factor …

Dicyclic and Tricyclic Diaminopyrimidine Derivatives as Potent Inhibitors of Cryptosporidium parvum Dihydrofolate Reductase: Structure-Activity and Structure …

RG Nelson, A Rosowsky - Antimicrobial agents and …, 2001 - Am Soc Microbiol
ABSTRACT A structurally diverse library of 93 lipophilic di-and tricyclic diaminopyrimidine
derivatives was tested for the ability to inhibit recombinant dihydrofolate reductase (DHFR) …

Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged …

A Rosowsky, V Cody, N Galitsky, H Fu… - Journal of medicinal …, 1999 - ACS Publications
As part of a larger search for potent as well as selective inhibitors of dihydrofolate reductase
(DHFR) enzymes from opportunistic pathogens found in patients with AIDS and other …

Resistance as a tool in the study of old and new drug targets in Toxoplasma

DC McFadden, M Camps, JC Boothroyd - Drug Resistance Updates, 2001 - Elsevier
Drug resistance generated in vitro in the protozoan parasite Toxoplasma gondii is
described. We focus on drugs that are in use in patients, that show some promise for such …