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- Revealing PACMA 31 as a new chemical type TrxR inhibitor to . . .
Propionic acid carbamoyl methyl amides (PACMAs) were early reported as protein disulfide isomerase (PDI) inhibitors against a set of human cancer cell lines Of note, PACMA 31 with excellent oral bioavailability exhibits high cytotoxicity and selectivity to cancer cells, especially in mouse xenograft models of human ovarian cancer [27], [28], [29]
- Discovery of an orally active small-molecule irreversible . . .
Among these molecules, PACMA 31 (bold numbers are used to indicate compounds) exhibited in vivo activity with oral bioavailability in a mouse xenograft model of human ovarian cancer PACMA 31 is an orally active small-molecule PDI inhibitor with desirable pharmacological properties for cancer treatment Most importantly, this study shows that
- Critical Evaluation of Human Oral Bioavailability for . . .
Oral bioavailability (%F) is a key factor that determines the fate of a new drug in clinical trials Traditionally, %F is measured using costly and time -consuming experimental tests Developing computational models to evaluate the %F of new drugs before they are synthesized would be beneficial in the drug discovery process
- PACMA 31 | Protein Disulfide Isomerase Inhibitor - MedChemExpress
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM PACMA 31 forms a covalent bond with the active site cysteines of PDI PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo
- PACMA-31 - Drug Targets, Indications, Patents - Synapse - Patsnap
The enzyme is considered a potential target for treating thrombosis We previously developed a potent PDI inhibitor, CPD, which contains the propiolamide as a warhead targeting cysteine residue in PDI To address its issues with undesirable off-target effects and weak metabolic stability, we replaced the propiolamide group with various
- Optimizing Oral Bioavailability in Drug Discovery: An . . .
In one example, the oral bioavailability of a poorly water soluble drug candidate was increased approximately 10-fold when administered to dogs as a solution using a mixture of cosolvents and surfactants, compared with that using a prototype solid formulation prepared with micronized drug substance 31 Similarly, the oral bioavailability of a
- Advances in Predictions of Oral Bioavailability of Candidate . . .
The following are available online, Figure S1: Observed oral bioavailability in man vs mouse, rat and dog, Table S1: Predicted and observed oral bioavailability (F) in man for the selected compounds, Table S2: Compounds excluded beforehand for prediction of oral bioavailability (F) and their predicted and observed fraction absorbed (f abs)
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