(±)-E-Homocamptothecin - CAS 186668-40-6
Category: Inhibitor
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Molecular Formula:
C21H18N2O4
Molecular Weight:
362.38
COA:
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Targets:
Topoisomerase
Description:
(±)-E-Homocamptothecin is a potent topoisomerase I (Topo 1) inhibitor.
Brife Description:
topoisomerase I (Topo 1) inhibitor
Purity:
99%
Synonyms:
(+/-)-E-Homocamptothecin; BN-80245; BN 80245; BN80245; E-Homocamptothecin, (+/-)-
MSDS:
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InChIKey:
PAEZRCINULFAGO-UHFFFAOYSA-N
InChI:
InChI=1S/C21H18N2O4/c1-2-21(26)9-18(24)27-11-14-15(21)8-17-19-13(10-23(17)20(14)25)7-12-5-3-4-6-16(12)22-19/h3-8,26H,2,9-11H2,1H3
Canonical SMILES:
CCC1(CC(=O)OCC2=C1C=C3C4=NC5=CC=CC=C5C=C4CN3C2=O)O
1.Homocamptothecin, an E-ring-modified camptothecin, exerts more potent antiproliferative activity than other topoisomerase I inhibitors in human colon cancers obtained from surgery and maintained in vitro under histotypical culture conditions.
Philippart P;Harper L;Chaboteaux C;Decaestecker C;Bronckart Y;Gordover L;Lesueur-Ginot L;Malonne H;Lavergne O;Bigg DC;da Costa PM;Kiss R Clin Cancer Res. 2000 Apr;6(4):1557-62.
Topoisomerase I (Topo I) is overexpressed in cancer colon tissues compared with normal colon tissues. Several anti-Topo I inhibitors are already successfully used in the clinic. We illustrate here the antiproliferative activity of a new class of Topo I inhibitors, i.e., E-ring-modified camptothecins with enhanced lactone stability (L. Lesueur-Ginot et al., Cancer Res., 59: 2939-2943, 1999). Forty-three human colon cancers were obtained from surgical resection and maintained under organotypical culture conditions for 48 h. Cell proliferation was assessed in these ex vivo tumor tissue cultures by tritiated thymidine autoradiography. As a validation of the methodology, we first analyzed in our model the antiproliferative activity of two clinically active topoisomerase II (Topo II) inhibitors, Adriamycin and etoposide, which are not active for colon cancers; and three Topo I inhibitors, camptothecin (CPT) and two clinically active compounds (especially for colon cancers), i.e., topotecan and the active metabolite of irinothecan, SN-38. We then compared the antiproliferative activity of CPT, topotecan, and SN-38 against those of two investigational E-ring-modified camptothecins, i.e., BN80245 and BN80915.
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CAS 186668-40-6 (±)-E-Homocamptothecin

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