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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

TRIP13

Action

inhibitors

Mechanism

TRIP13 inhibitors(thyroid hormone receptor interactor 13 inhibitors)

Therapeutic Areas

NeoplasmsImmune System DiseasesCardiovascular Diseases+ [1]

Active Indication

Multiple Myeloma

Inactive Indication-

Originator Organization

Technical Institute of Physics & Chemistry CAS

Active Organization

Technical Institute of Physics & Chemistry CAS

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

This study reported the design and synthesis of novel 1-amido-2-one-4-thio-deoxypyranose as inhibitors of potential drug target TRIP13 for developing new mechanism-based therapeutic agents in the treatment of multiple myeloma (MM).In comparison with the pos. control DCZ0415, the most active compounds C16, C18, C20 and C32 exhibited strong anti-proliferative activity against human MM cell lines (ARP-1 and NCI-H929) with IC₅₀ values of 1 ∼ 2μM.While the surface plasmon resonance (SPR) and ATPase activity assays demonstrated that the representative compound C20 is a potent inhibitor of TRIP13, C20 also showed good antitumor activity in vivo on BALB/c nude mice xenografted with MM tumor cells.An initial structure-activity study showed that the carbonyl group is crucial for anticancer activity.Overall, this study provided novel 1-amido-2-one-4-thio-deoxypyranoses, which are entirely different from previously reported potent inhibitor structures of TRIP13, and thus would aid the development of carbohydrate-based novel agents in MM pharmacotherapy.

100 Deals associated with C20(Technical Institute of Physics & Chemistry CAS)

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