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Your search keyword '"Farnesylthiosalicylic acid"' showing total 2 results
Start Over Descriptor "Farnesylthiosalicylic acid" Publisher american chemical society (acs)
2 results on '"Farnesylthiosalicylic acid"'

1. Mediated Imaging and Improved Targeting of Farnesylthiosalicylic Acid Delivery for Pancreatic Cancer via Conjugation with Near-Infrared Fluorescence Heptamethine Carbocyanine Dye

Author

Caiqin Zhang, Yong Zhao, He Zhang, Pengpeng Wu, Jiaze An, Ya Zhao, Changhong Shi, Dengxu Tan, Jie Wang, and Bing Bai

Subjects
Biomaterials, Ras Inhibitor, Chemistry, Pancreatic cancer, Biochemistry (medical), Biomedical Engineering, medicine, Cancer research, General Chemistry, Near infrared fluorescence, medicine.disease, Farnesylthiosalicylic acid
Abstract

S-trans–trans-Farnesylthiosalicylic acid (FTS) is a Ras inhibitor that exhibits desirable anticancer property and currently undergoing clinical trials for pancreatic cancer (PC). However, its poor ...

Published
2020

2. New Derivatives of Farnesylthiosalicylic Acid (Salirasib) for Cancer Treatment: Farnesylthiosalicylamide Inhibits Tumor Growth in Nude Mice Models

Author

Aaron Heiss, Victor J. Bauer, Liat Goldberg, Roni Haklai, and Yoel Kloog

Subjects
MAP Kinase Signaling System, Mice, Nude, Antineoplastic Agents, Growth inhibitory, Oncogene Protein p21(ras), Mice, chemistry.chemical_compound, Cell Line, Tumor, Neoplasms, Amide, Drug Discovery, Animals, Humans, Tumor growth, Enzyme Inhibitors, Extracellular Signal-Regulated MAP Kinases, Ras Inhibitor, Molecular Structure, Cell growth, Amides, Cyclic AMP-Dependent Protein Kinases, Farnesol, Xenograft Model Antitumor Assays, Farnesylthiosalicylic acid, Salicylates, Cancer treatment, Disease Models, Animal, chemistry, Biochemistry, Disease Progression, Molecular Medicine, Selectivity
Abstract

The Ras inhibitor S-trans,trans-farnesylthiosalicylic acid (FTS, Salirasib) interferes with Ras membrane interactions that are crucial for Ras-dependent transformation. It remains unknown whether modifications of the carboxyl group of FTS can affect its activity. Here we show that specific modifications of the FTS carboxyl group by esterification or amidation yield compounds with improved growth inhibitory activity, compared to FTS, as shown in Panc-1 and U87 cells. The most potent compounds were FTS-methoxymethyl ester and FTS-amide. However, selectivity toward active Ras-GTP, as known for FTS, was apparent with the amide derivatives of FTS. FTS-amide exhibited the overall highest efficacy in inhibition of Ras-GTP and cell growth. This new compound significantly inhibited growth of both Panc-1 tumors and U87 brain tumors. Thus amide derivatives of the FTS carboxyl group provide potent cell-growth inhibitors without loss of selectivity toward the active Ras protein and may serve as new candidates in cancer therapy.

Published
2008

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