LY231514, a pyrrolo [2, 3-d] pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes

…, DJ Soose, VF Patel, SL Andis, JR Bewley… - Cancer research, 1997 - AACR
N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]-benzoyl]-l-glutamic
acid (LY231514) is a novel pyrrolo[2,3-d]pyrimidine-based antifolate currently undergoing …

Sulfonimidamide Analogs of Oncolytic Sulfonylureas,1

…, JE Ray, GB Boder, JR Bewley… - Journal of medicinal …, 1997 - ACS Publications
A series of sulfonimidamide analogs of the oncolytic diarylsulfonylureas was synthesized and
evaluated for (1) in vitro cytotoxicity against CEM cells, (2) in vivo antitumor activity against …

Biological activity of the multitargeted antifolate, MTA (LY231514), in human cell lines with different resistance mechanisms to antifolate drugs.

RM Schultz, VJ Chen, JR Bewley, EF Roberts… - Seminars in …, 1999 - europepmc.org
Prior studies have indicated that MTA requires intracellular polyglutamation for optimal
cytotoxic effect and that these polyglutamates potently inhibit several key enzymes of folate …

Augmentation of the Therapeutic Activity of Lometrexol [(6-R)5,10-Dideazatetrahydrofolate] by Oral Folic Acid

T Alati, JF Worzalla, C Shih, JR Bewley, S Lewis… - Cancer research, 1996 - AACR
Recent clinical trials with lometrexol [(6R)-5,10-dideazatetrahydrofolate] have revealed a
level of toxicity in humans that was not predicted on the basis of previous in vivo preclinical …

The antiproliferative and cell cycle effects of 5, 6, 7, 8-tetrahydro-N5, N10-carbonylfolic acid, an inhibitor of methylenetetrahydrofolate dehydrogenase, are potentiated …

…, LL Habeck, JE Toth, LG Mendelsohn, J Bewley… - … of Pharmacology and …, 1998 - ASPET
5,6,7,8-Tetrahydro-N 5 ,N 10 -carbonylfolic acid (LY354899) has been demonstrated to
inhibit the dehydrogenase activity of C1-tetrahydrofolate synthase. This compound was only …

Comparison of metabolism and toxicity to the structure of the anticancer agent sulofenur and related sulfonylureas

…, JM Woodland, JF Worzalla, JR Bewley… - Chemical research in …, 1992 - ACS Publications
The metabolic formation of p-chloroaniline from the oncolytic agent sulofenur [N-(5-indanesulfonyl)-iV,-(4-chlorophenyl)
urea, LY186641, 1] and from similar diaryl-substituted …

Cellular pharmacology of MTA: a correlation of MTA-induced cellular toxicity and in vitro enzyme inhibition with its effect on intracellular folate and nucleoside …

VJ Chen, JR Bewley, SL Andis… - Seminars in …, 1999 - pubmed.ncbi.nlm.nih.gov
The mechanism of action of an antifolate may be investigated using a variety of experimental
methods. These include experiments in a cell culture setting to observe possible protection …

Automated measurement of transplantable solid tumors using digital electronic calipers interfaced to a microcomputer

JF Worzalla, JR Bewley, GB Grindey - Investigational new drugs, 1990 - Springer
Data collection for transplantable solid tumors has been automated with electronic digital
calipers and a balance which have been coupled through an RS-232 interface to a …

Pharmacokinetics of the anticancer agent sulofenur in mice, rats, monkeys, and dogs

…, GB Grindey, JF Worzalla, JR Bewley… - Journal of …, 1993 - Elsevier
The absorption and pharmacokinetics of sulofenur [N-(in- dan-5-sulfonyl)-N-(4-chlorophenyl)urea,
LY186641] and its major metabolites were examined in mice, rats, monkeys, and dogs…

Medicinal chemistry of difluoropurines.

SL Andis, JR Bewley, GB Boder, T Burke… - Seminars in …, 1995 - europepmc.org
A series of over 70 difluoropurine analogs was synthesized by varying the C-2, 6 and 8
substituents about the purine ring system. After initial in vitro and in vivo screening, testing …