SARDOMOZIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C11H14N6
Molecular Weight	230.2691
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

NC(=N)N\N=C1/CCC2=C(C=CC=C12)C(N)=N

InChI

InChIKey=CYPGNVSXMAUSJY-CXUHLZMHSA-N

InChI=1S/C11H14N6/c12-10(13)8-3-1-2-7-6(8)4-5-9(7)16-17-11(14)15/h1-3H,4-5H2,(H3,12,13)(H4,14,15,17)/b16-9+

HIDE SMILES / InChI

Molecular Formula	C11H14N6
Molecular Weight	230.2691
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9078276 | https://www.ncbi.nlm.nih.gov/pubmed/14977828 | https://adisinsight.springer.com/drugs/800004127

Sardomozide (previously known as SAM486A or CGP-48664) was developed as an inhibitor of S-adenosyl-methionine-decarboxylase, a key enzyme for polyamine biosynthesis. Sardomozide possessed the broad-spectrum antiproliferative and antitumor activity. The drug participated in a phase II clinical trial as a monotherapy in patients with refractory or relapsed non-Hodgkin's lymphoma. In Phase II clinical trial in patients with metastatic melanoma, the drug didn’t have significant therapeutic potential. The further development of this drug was discontinued.

Originator

Approval Year

PubMed

Title	Date	PubMed
4-Amidinoindan-1-one 2'-amidinohydrazone: a new potent and selective inhibitor of S-Adenosylmethionine decarboxylase.	1993 Jul 23	8340919
CGP 48664, a potent and specific S-adenosylmethionine decarboxylase inhibitor: effects on regulation and stability of the enzyme.	1997 Feb 15	9078276
Inhibition of multidrug-resistant HIV-1 by interference with cellular S-adenosylmethionine decarboxylase activity.	2006 Sep 15	16941339
Inhibition of S-adenosylmethionine decarboxylase by inhibitor SAM486A connects polyamine metabolism with p53-Mdm2-Akt/protein kinase B regulation and apoptosis in neuroblastoma.	2009 Jul	19584241

Patents

Sample Use Guides

In Vivo Use Guide

Forty-one previously treated patients with either diffuse large cell, follicular, or peripheral T-cell NHL were treated i.v. with 100 mg/m(2) SAM486A (SARDOMOZIDE) as a daily 1-h infusion for 5 days repeated every 3 weeks. Treatment was continued for a total of eight cycles or until disease progression.

Route of Administration: Intravenous

Substance Class	Chemical Created by `admin` on `Sat Dec 16 16:20:13 GMT 2023` Edited by `admin` on `Sat Dec 16 16:20:13 GMT 2023`
Record UNII	CEB05S0B9I
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SARDOMOZIDE

Official Name

English

4-(AMINOIMINOMETHYL)-2,3-DIHYDRO-1H-INDEN-1-ONE-DIAMINOMETHYLENEHYDRAZONE

Systematic Name

English

sardomozide [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C2076