Delving into the Latest Updates on Taxoid 15 b with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

β-tubulin

Action

inhibitors

Mechanism

β-tubulin inhibitors(tubulin beta class I inhibitors)

Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication-

Originator Organization

Chinese Academy of Medical Sciences

Active Organization

Chinese Academy of Medical Sciences

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

AbstractA series of C2‐modified 10‐deacetyl‐7‐propionyl cephalomannine derivatives was designed, prepared, and biologically evaluated. Some C2 meta‐substituted benzoate analogues showed potent activity against both drug‐sensitive and drug‐resistant tumor cells in which resistance is mediated through either P‐gp overexpression or β‐tubulin mutation mechanisms. The taxoid 15 b and related compounds are of particular interest, as they are much more cytotoxic than paclitaxel, especially against drug‐resistant tumor cells; they are able to kill both drug‐resistant and drug‐sensitive cells (low R/S ratio), and they have high affinity for β‐tubulin. Our research results led to an important hypothesis, that is, a taxane with very high binding affinity for β‐tubulin is able to counteract drug resistance, which may assist in future taxane‐based drug‐discovery efforts.

100 Deals associated with Taxoid 15 b

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