15 research outputs found
Synthesis of bilocularin A carbamate derivatives and their evaluation as leucine transport inhibitors in prostate cancer cells
No full textIdentification of Gibberellic Acid Derivatives That Deregulate Cholesterol Metabolism in Prostate Cancer Cells
No full textThe naturally occurring pentacyclic
diterpenoid gibberellic acid
(<b>1</b>) was used in the generation of a drug-like amide library
using parallel-solution-phase synthesis. Prior to the synthesis, a
virtual library was generated and prioritized based on drug-like physicochemical
parameters such as log P, hydrogen bond donor/acceptor counts, and
molecular weight. The structures of the synthesized analogues (<b>2</b>–<b>13</b>) were elucidated following analysis
of the NMR, MS, UV, and IR data. Compound <b>12</b> afforded
crystalline material, and its structure was confirmed by X-ray crystallographic
analysis. All compounds were evaluated <i>in vitro</i> for
cytotoxicity and deregulation of lipid metabolism in LNCaP prostate
cancer cells. While no cytotoxic activity was identified at the concentrations
tested, synthesized analogues <b>3</b>, <b>5</b>, <b>7</b>, <b>10</b>, and <b>11</b> substantially reduced
cellular uptake of free cholesterol in prostate cancer cells, suggesting
a novel role of gibberellic acid derivatives in deregulating cholesterol
metabolism
Multimodal γ′ precipitation in Inconel-738 Ni-based superalloy during electron-beam powder bed fusion additive manufacturing
No full textHot cracking in pulsed laser processing of a nickel based superalloy built up by electrospark deposition
No full textTransient-Liquid-Phase Bonding of H230 Ni-Based Alloy Using Ni-P Interlayer: Microstructure and Mechanical Properties
No full textCrack Growth Modeling and Life Prediction of Pipeline Steels Exposed to Near-Neutral pH Environments: Dissolution Crack Growth and Occurrence of Crack Dormancy in Stage I
No full textNew approach for assessing the weldability of precipitation-strengthened nickel-base superalloys
No full text
