220998-10-7
Chemical Structure
Elomotecan
Synonym(s): BN 80927 free base
- CAS No.: 220998-10-7
- Formula:C29H32ClN3O4
- Molecular Weight:522.04
IUPAC Name: (R)-9-chloro-5-ethyl-5-hydroxy-10-methyl-12-((4-methylpiperidin-1-yl)methyl)-1,4,5,13-tetrahydro-3H,15H-oxepino[3',4':6,7]indolizino[1,2-b]quinoline-3,15-dione
InChIKey: KAQREZSTQZWNAG-GDLZYMKVSA-N
SMILES: O=C(OC1)C[C@](O)(CC)C2=C1C(N3CC4=C(CN5CCC(C)CC5)C6=CC(C)=C(Cl)C=C6N=C4C3=C2)=O
Biological Activity: Elomotecan (BN 80927 free base) is an orally active, potent inhibitor of topoisomerases I and II and a homocamptothecin (hCPT) analogue. Elomotecan possesses a dual inhibitory mechanism: it acts as a topoisomerase I poison by stabilizing the DNA-enzyme complex while simultaneously serving as a catalytic inhibitor of topoisomerase II. Elomotecan is used in research concerning various advanced and multidrug-resistant (MDR) solid tumors (such as prostate, colon, and breast cancers)[1][2][3][4].
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Elomotecan | Elomotecan (BN 80927 free base) is an orally active, potent inhibitor of topoisomerases I and II and a homocamptothecin (hCPT) analogue. Elomotecan possesses a dual inhibitory mechanism: it acts as a topoisomerase I poison by stabilizing the DNA-enzyme complex while simultaneously serving as a catalytic inhibitor of topoisomerase II. Elomotecan is used in research concerning various advanced and multidrug-resistant (MDR) solid tumors (such as prostate, colon, and breast cancers). | |||||||||||||||||||||
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References
- [1]. Demarquay D, et al. BN80927: a novel homocamptothecin that inhibits proliferation of human tumor cells in vitro and in vivo. Cancer Res. 2004 Jul 15;64(14):4942-9. [Content Brief]
- [2]. Trocóniz IF, et al. Population pharmacokinetic/pharmacodynamic modeling of drug-induced adverse effects of a novel homocamptothecin analog, elomotecan (BN80927), in a Phase I dose finding study in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2012 Aug;70(2):239-50. [Content Brief]
- [3]. Huchet M, et al. The dual topoisomerase inhibitor, BN 80927, is highly potent against cell proliferation and tumor growth. Ann N Y Acad Sci. 2000;922:303-5. [Content Brief]
- [4]. Demarquay D, et al. The homocamptothecin, BN 80927, is a potent topoisomerase I poison and topoisomerase II catalytic inhibitor. Ann N Y Acad Sci. 2000;922:301-2. [Content Brief]
