Delving into the Latest Updates on Ketocaine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target-

Mechanism-

Therapeutic Areas

NeoplasmsNervous System Diseases

Active Indication-

Inactive Indication

NeoplasmsPainPrimary dysmenorrhea

Originator Organization

Recordati SpA

AstraZeneca PLC

Active Organization-

Inactive Organization

University of Lund

Alma Mater Studiorum - Università di Bologna

University of Oulu

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC18H29NO2

InChIKeyUXAWFWFJXIANHZ-UHFFFAOYSA-N

CAS Registry1092-46-2

The synthesis of two nitrogen mustard derivatives (VIII and IX) related to the well-known local anesthetic ketocaine (III) is reported. These compounds were tested in mice implanted with Ehrlich ascites tumor cells, and the antitumor activity was compared with that of two previously synthesized analogues (I and II) lacking the nitro group and with that of doxorubicin. The monofunctional compound IX was inactive, but the bifunctional compound VIII showed potent antitumor activity (%T/C greater than 254 at 20 mg/kg).

01 Jan 1984·Archiv der PharmazieQ4 · MEDICINE

Potential Antitumor Agents, XXII. Alkylating Agents from p‐Hydroxypropiophenone and p‐Hydroxyacetophenone

Q4 · MEDICINE

Article

Author: Daniela Bonazzi ; Rosaria Bossa ; Giovanna Lelli ; Mirella Rambaldi ; Aldo Andreani ; Iraklis Galatulas

Abstract:

The synthesis of the alkylating agents 18–25 from p‐hydroxypropiophenone, p‐hydroxyacetophenone and their nitro derivatives 14–17 is reported. The antitumor activities of these new compounds are compared to those of the previously reported analogs 2–13 of the local anesthetic ketocaine (1).

01 Jul 1983·Journal of pharmaceutical sciencesQ3 · MEDICINE

Potential Antitumor Agents IX: Synthesis and Antitumor Activity of Two Analogues of Ketocaine

Q3 · MEDICINE

Article

Author: Rosaria Bossa ; Giancarlo Scapini ; Iraklis Galatulas ; Aldo Andreanix

The reaction between o-hydroxybutyrophenone and tris(2-chloroethyl)amine gave two analogues (II, V) of the well-known local anesthetic ketocaine (I). Compounds II and V showed interesting antitumor activity in mice implanted with Ehrlich ascites tumor cells (% T/C = 149 at 5 mg/kg and 171 at 50 mg/kg, respectively). Further studies on the pharmacological behavior of these new compounds are in progress.

100 Deals associated with Ketocaine

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Preclinical	IT	Alma Mater Studiorum - Università di Bologna	01 Aug 1984
Pain	Preclinical	FI	University of Oulu	01 Jan 1983
Primary dysmenorrhea	Preclinical	SE	University of Lund	01 Jan 1980