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.

2008-01-01·Gynecologic and Obstetric Investigation4区 · 医学

A Universal Combination Treatment for Vaginitis

4区 · 医学

Article

作者: 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.

2006-02-01·Cancer Chemotherapy and Pharmacology4区 · 医学

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

4区 · 医学

Article

作者: 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 项与 4-Demethylpenclomedine 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB06331

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
肿瘤	临床1期	-	Southern Research Institute	-
肿瘤	临床1期	-	The Johns Hopkins University	-
肿瘤	临床1期	-	Antisoma, Inc.	-
实体瘤	临床1期	美国	-	-