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Intrinsic and acquired forms of resistance against the anticancer ruthenium compound KP1019 [indazolium trans-[tetrachlorobis(1H-indazole)ruthenate (III)] (FFC14A).

Institute of Cancer Research
Syntheses and thymidylate synthase inhibitory activity of the poly-gamma-glutamyl conjugates of N-[5-[N-(3,4-dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N-methylamino ]-2-thenoyl]-L-glutamic acid (ICI D1694) and other quinazoline antifolates.

Institute of Cancer Research
Analogues of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity.

Institute of Cancer Research
The 16,17-double bond is needed for irreversible inhibition of human cytochrome p45017alpha by abiraterone (17-(3-pyridyl)androsta-5, 16-dien-3beta-ol) and related steroidal inhibitors.

Institute of Cancer Research
Studies on selectin blocker. 1. Structure-activity relationships of sialyl Lewis X analogs.

Institute of Cancer Research
The synthesis and thymidylate synthase inhibitory activity of L-gamma-L-linked dipeptide and L-gamma-amide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).

Institute of Cancer Research
Dinucleotide analogues as inhibitors of thymidine kinase, thymidylate kinase, and ribonucleotide reductase.

Institute of Cancer Research
Discovery of 2-(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes.

Institute of Cancer Research
Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.

Institute of Cancer Research
Novel fluorinated prodrugs for activation by carboxypeptidase G2 showing good in vivo antitumor activity in gene-directed enzyme prodrug therapy.

Institute of Cancer Research
Solid-phase synthesis of novel inhibitors of farnesyl transferase.

Institute of Cancer Research
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.

Institute of Cancer Research
Mustard prodrugs for activation by Escherichia coli nitroreductase in gene-directed enzyme prodrug therapy.

Institute of Cancer Research
Quinazoline antifolate thymidylate synthase inhibitors: gamma-linked L-D, D-D, and D-L dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).

Institute of Cancer Research
Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer.

Institute of Cancer Research
Homologs of idoxifene: variation of estrogen receptor binding and calmodulin antagonism with chain length.

Institute of Cancer Research
Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.

Institute of Cancer Research
Quinazoline antifolates inhibiting thymidylate synthase: 2-desamino derivatives with enhanced solubility and potency.

Institute of Cancer Research
Crystallographic and molecular modeling studies on 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione and its butyl analogue, inhibitors of mammalian aromatase. Comparison with natural substrates: prediction of enantioselectivity for N-alkyl derivatives.

Institute of Cancer Research
Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis.

Institute of Cancer Research
Quinazoline antifolate thymidylate synthase inhibitors: 2'-fluoro-N10-propargyl-5,8-dideazafolic acid and derivatives with modifications in the C2 position.

Institute of Cancer Research
Inhibition of enzymes of estrogen and androgen biosynthesis by esters of 4-pyridylacetic acid.

Institute of Cancer Research
Quinazoline antifolates inhibiting thymidylate synthase: 4-thio-substituted analogues.

Institute of Cancer Research
Quinazoline antifolate thymidylate synthase inhibitors: difluoro-substituted benzene ring analogues.

Institute of Cancer Research
Conformational analysis of the aromatase inhibitor 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione (rogletimide) and discovery of potent 5-alkyl derivatives.

Institute of Cancer Research
A novel mechanism by which small molecule inhibitors induce the DFG flip in Aurora A.

Moffitt Cancer Center