ROGLETIMIDE

Details

Stereochemistry	RACEMIC
Molecular Formula	C12H14N2O2
Molecular Weight	218.2518
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCC1(CCC(=O)NC1=O)C2=CC=NC=C2

InChI

InChIKey=QXKJWHWUDVQATH-UHFFFAOYSA-N

InChI=1S/C12H14N2O2/c1-2-12(9-4-7-13-8-5-9)6-3-10(15)14-11(12)16/h4-5,7-8H,2-3,6H2,1H3,(H,14,15,16)

HIDE SMILES / InChI

Molecular Formula	C12H14N2O2
Molecular Weight	218.2518
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/1419608 | https://www.ncbi.nlm.nih.gov/pubmed/7949204

Rogletimide (pyridoglutethimide) is a second-generation nonsteroidal aromatase inhibitor that has been evaluated for use in the treatment of breast cancer. Rogletimide is a structural analog of aminoglutethimide (AG), a nonspecific aromatase inhibitor. Roglemitide is slightly less potent than AG but does not inhibit the cholesterol side-chain cleavage and shows no sedative activity. However, compared to AG, it has sub-optimal aromatase inhibition and oestradiol suppression.

Approval Year

PubMed

Title	Date	PubMed
FACE: the barefaced facts of AI potency.	2010-10-27	21188118
The what, why and how of aromatase inhibitors: hormonal agents for treatment and prevention of breast cancer.	2007-12	17892469
Aromatase inhibition in the treatment of advanced breast cancer: is there a relationship between potency and clinical efficacy?	2004-05-04	15150604
Professor Tom Connors and the development of novel cancer therapies by the Phase I/II Clinical Trials Committee of Cancer Research UK.	2003-08-04	12888809
Stereoselective determination of pyridoglutethimide enantiomers in serum with a chiral cellulose-based high-performance liquid chromatographic column using solid phase extraction and UV detection.	2003-04-01	12684112
The effect of the aromatase inhibitor, rogletimide (pyridoglutethimide), on guinea pig adrenal cell steroidogenesis and placental microsomal aromatase activity: comparison with aminoglutethimide and CGS 16949A.	1991-11	1659868

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:11:34 GMT 2025` Edited by `admin` on `Mon Mar 31 18:11:34 GMT 2025`
Record UNII	14P4QR28QF
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ROGLETIMIDE

Official Name

English

(±)-PYRIDOGLUTETHIMIDE

Preferred Name

English

Rogletimide [WHO-DD]

Common Name

English

2,6-PIPERIDINEDIONE, 3-ETHYL-3-(4-PYRIDINYL)-

Systematic Name

English

rogletimide [INN]

Common Name

English

ROGLETIMIDE [USAN]

Common Name

English

PYRIDOGLUTETHIMIDE

Common Name

English

ROGLETIMIDE [MART.]

Common Name

English

(±)-2-ETHYL-2-(4-PYRIDYL)GLUTARIMIDE

Systematic Name

English

2,6-PIPERIDINEDIONE, 3-ETHYL-3-(4-PYRIDINYL)-, (±)-

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C2018