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Restrict the search for
uracil mustard
to a specific field?
Status:
Investigational
Source:
NCT00769288: Phase 1 Interventional Completed Adult Grade III Lymphomatoid Granulomatosis
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
1-(2-DEOXY-2-FLUORO-β-D-ARABINOFURANOSYL)URACIL (FAU) is a thymidine analog. In several cancer cell lines, FAU was phosphorylated intracellularly to its monophosphate, 1-(2-deoxy-2-fluoro--Darabinofuranosyl) uracil monophosphate (FAUMP), by thymidine kinase and methylated in the 5-position by thymidylate synthase to form the product, 1-(2-deoxy-2-fluoro- -D-arabinofuranosyl) 5-methyluracil monophosphate (FMAUMP). FAU strongly inhibits the growth of tumor cells with high thymidylate synthase activity. FAU had been in phase I clinical trial for the treatment of advanced solid tumors.
Class (Stereo):
CHEMICAL (ACHIRAL)
Tallimustine (also known as FCE 24517), an alkylating benzoyl mustard derivative of distamycin A that was studied as an anti-tumor agent. Tallimustine participated in phase I clinical trial in patients with advanced cancer. As a result, the was obtained the recommended Phase II dosage for tallimustine. However, the further development of this drug was discontinued.
Status:
Investigational
Source:
INN:metamelfalan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Metamelfalan is an antineoplastic agent. Metamelfalan is the meta form of the levo isomer melphalan. Metamelfalan causes crosslinking of DNA, thereby preventing DNA replication and eventually cellular proliferation.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Netivudine [882C, 882C87, BW 882, Py-araU, Zonavir®] is an orally active thymidine analogue which was being investigated as a treatment for herpes zoster virus infections. Netivudine is a nucleoside analog with potent, specific activity against varicella-zoster virus. It is approximately seven times as potent as acyclovir with an in vitro 50% inhibitory concentration of 1 to 2 uM.
Status:
Investigational
Source:
INN:galamustine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Galamustine (C6-galactose mustard or C6-GLM ) is a compound that has demonstrated anti-cancer activity. Its effect on cell growth and cell cycle kinetics was studied in leukemia. Because less bone marrow toxicity was reported for this compound compared to nitrogen mustard, the development of galamustine for clinical trials in humans was considered.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Alestramustine is the l-alanine ester form of estramustine, a combination of the nitrogen mustard normustine coupled via a carbamate to estradiol, with antineoplastic activity. Upon conversion of alestramustine to estramustine, estramustine binds to microtubule-associated proteins (MAPs) and beta tubulin, thereby interfering with microtubule dynamics and leading to microtubule disassembly and cell cyle arrest. Due to the estrogen moiety, this agent is able to selectively bind to and be taken up by estrogen receptor-positive cells.
Class (Stereo):
CHEMICAL (ACHIRAL)
Mitoclomine, an alkylating agent was developed to treat cancer. This drug was involved in phase I/II clinical trial to treat patients with chronic lymphocytic leukemia. Information about the further development of a drug is not available.
Class (Stereo):
CHEMICAL (EPIMERIC)
Bofumustine, also known as RFCNU was studied as an antitumor agent. Bofumustine participated in phase II trials in patients with digestive tract tumors. It was shown that 30% has remissions among which 13% were greater than 50%. In addition, bofumustine participated in phase II clinical trials, where it showed to be effective in 8% of digestive tumors, in 1 out of 7 pancreatic cancers and in 3 out of 10 hepatic and pulmonary metastases from an undiscovered primary adenocarcinoma. However, further information is not available.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Sarcolysin is the isomeric form of melphalan with alkylating activity. Sarcolysin is a bifunctional alkylating agent. The cytotoxicity of sarcolysin appears to be related to the extent of its interstrand cross-linking with DNA, probably by binding at the N7 position of guanine. Like other bifunctional alkylating agents, it is active against both resting and rapidly dividing tumor cells. The levo-isomer - melphalan (L-sarcolysin) is approved under the brand name ALKERAN for the palliative treatment of multiple myeloma and for the palliation of non-resectable epithelial carcinoma of the ovary. In addition, the drug was approved under the trade name Evomela. Evomela is indicated for use as a high-dose conditioning treatment prior to hematopoietic progenitor (stem) cell transplantation in patients with multiple myeloma. In addition, for the palliative treatment of patients with multiple myeloma for whom oral therapy is not appropriate.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ambamustine (PTT-119) is a bifunctional alkylating agent. Its antitumour effect is reported to mainly be through alkylation and interstrand cross-linkage of DNA. The drug was awaiting registration in Italy for the treatment of non-Hodgkin's lymphoma, and was also in phase-II clinical trial for small cell lung cancer, but was discontinued.
