PURPOSEThe purpose of this investigation was to synthesize a series of carbonate and carbamate derivatives of 4-demethylpenclomedine (DM-PEN), the major plasma non-toxic metabolite of penclomedine (PEN) seen in patients. DM-PEN has been observed to be an active antitumor agent in mouse human xenograft tumor models and non-neurotoxic in a rat model, however, activity in intracranially implanted human glioma xenograft models have not been reported. The major goal was to identify derivatives that are active in brain tumors.METHODSDerivatives were prepared from DM-PEN and evaluated in vivo against human U251 glioblastoma, D54 glioblastoma and MX-1 breast tumor xenografts and mammary tumor 16/C that were implanted in the mammary fat pad or intracranially (IC).RESULTSCarbonate and carbamate derivatives were found to be superior to DM-PEN against IC growing human glioblastoma xenografts.CONCLUSIONThe activity of the carbonates and carbamates against human tumor xenografts in vivo suggests consideration of these two series of derivatives of DM-PEN for clinical development.

01 Jan 2008·Gynecologic and Obstetric InvestigationQ4 · MEDICINE

A Universal Combination Treatment for Vaginitis

Q4 · MEDICINE

Article

Author: Zarfati, Doron ; Bornstein, Jacob

Background: We compared a novel vaginal tablet consisting of 100 mg of clotrimazole and 100 mg of metronidazole (‘Clo-Met’) to a 100-mg clotrimazole tablet in the treatment of vaginitis. Methods: A multicenter, double-blind, randomized controlled study. Women with vaginal discharge and diagnosed as suffering from vaginitis caused by Trichomonas vaginalis, bacterial vaginosis or Candida albicans, or any combination of the three, and who had not received treatment for vaginitis during the previous month, were studied. Results: 165 patients were enrolled into the study – 84 into the combined therapy group, and 81 into the clotrimazole group. In women with Candida vaginitis, Clo-Met was more effective than clotrimazole treatment (p < 0.012 and p < 0.05, respectively). Conclusion: A combination vaginal tablet consisting of clotrimazole and metronidazole is therapeutically effective in candidal vaginitis. The effectiveness of Clo-Met on bacterial vaginosis, T. vaginalis infection as well as on vaginal infections due to a combination of these microorganisms should be studied further.

01 Feb 2006·Cancer Chemotherapy and PharmacologyQ4 · MEDICINE

Thiolo-, thiono- and dithiocarbonate and thiocarbamate derivatives of demethylpenclomedine as novel anticancer agents

Q4 · MEDICINE

Article

Author: William R. Waud ; Robert F. Struck

PURPOSEThe purpose of this investigation was to synthesize a series of thiolo-, thiono- and dithiocarbonate and thiocarbamate derivatives of 4-demethylpenclomedine (DM-PEN), the major plasma metabolite of penclomedine (PEN) in patients observed subsequently to be an active antitumor agent and non-neurotoxic in a rat model, in order to compare their antitumor activity with that of DM-PEN.METHODSDerivatives were prepared from DM-PEN and evaluated in vivo against human MX-1 breast tumor xenografts implanted in the mammary fat pad, several of which were also evaluated against human brain tumor xenografts.RESULTSThiolocarbonate and thiocarbamate derivatives were found to be superior to DM-PEN against MX-1 tumor and modestly active against glioblastoma.CONCLUSIONThe activity of the thiolocarbonates and thiocarbamates against human tumor xenografts in vivo suggests consideration of these two series of derivatives of DM-PEN for clinical development.

100 Deals associated with 4-Demethylpenclomedine

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KEGG	Wiki	ATC	Drug Bank
-	-	-	DB06331

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Phase 1	-	Southern Research Institute	-
Neoplasms	Phase 1	-	The Johns Hopkins University	-
Neoplasms	Phase 1	-	Antisoma, Inc.	-
Solid tumor	Phase 1	United States	-	-

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