Details
Stereochemistry | EPIMERIC |
Molecular Formula | C35H33FN6O3 |
Molecular Weight | 604.6733 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCC[C@H]1CCNC(=O)C2=CN3C4=C(OC5=C3C(=CC(F)=C5N6CCC(C6)C7=CN=CC=N7)C2=O)C=C8C=CC=CC8=C4
InChI
InChIKey=WOQIDNWTQOYDLF-CGAIIQECSA-N
InChI=1S/C35H33FN6O3/c1-40-13-4-7-24(40)8-10-39-35(44)26-20-42-29-15-21-5-2-3-6-22(21)16-30(29)45-34-31(42)25(33(26)43)17-27(36)32(34)41-14-9-23(19-41)28-18-37-11-12-38-28/h2-3,5-6,11-12,15-18,20,23-24H,4,7-10,13-14,19H2,1H3,(H,39,44)/t23?,24-/m0/s1
Quarfloxin (also known as CX-3543) is a fluoroquinolone derivative patented by Cyclene Pharmaceuticals, Inc. as an antitumor agent. Quarfloxin selectively disrupts nucleolin/rDNA G-quadruplex complexes in the nucleolus, thereby inhibiting DNA polymerase I transcription and inducing apoptosis in cancer cells. CX-3543 was evaluated in phase II clinical studies for the treatment of low or intermediate grade neuroendocrine carcinoma, including carcinoid and islet cell cancer. In 2008, a trial for the treatment of chronic lymphocytic leukemia (CLL) was withdrawn prior to patient enrollment. In 2010, phase I clinical studies for the treatment of solid tumors and for the treatment of lymphoma were terminated upon the observation that the modified dose schedule presented no advantage over previously studies schedule solid tumors/ Cylene discontinued development of quarfloxin in 2010.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT00780663
IV Quarfloxin 240 mg/m2 daily x5 days every 21 days
Route of Administration:
Intravenous
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C274
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ACTIVE MOIETY