Page last updated: 2024-11-13

14-o-phosphonooxymethyltriptolide

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Description

## 14-O-Phosphonooxymethyltriptolide (14-OPT)

**What is it?**

14-OPT is a **synthetic derivative** of the naturally occurring compound **triptolide**, which is extracted from the Chinese herb **Tripterygium wilfordii**. It's a potent **immunosuppressant** with potential therapeutic applications in various fields.

**Key Characteristics:**

* **Chemical Structure:** 14-OPT differs from triptolide by having a phosphonooxymethyl group attached at the 14-position of the triptolide molecule.
* **Improved Properties:** This structural modification enhances its **pharmacokinetic properties** (how the body absorbs, distributes, metabolizes, and eliminates the drug), leading to improved **bioavailability**, **stability**, and **therapeutic index** compared to triptolide.

**Why is it important for research?**

14-OPT is of significant interest to researchers due to its promising potential in various areas, including:

**1. Treatment of Autoimmune Diseases:**

* **Mechanism of Action:** 14-OPT effectively **suppresses the immune system** by inhibiting the activity of various immune cells, including T cells, B cells, and macrophages. This makes it a potential candidate for treating autoimmune diseases like rheumatoid arthritis, lupus, and multiple sclerosis.
* **Clinical Trials:** Several clinical trials are underway to evaluate the efficacy and safety of 14-OPT in treating different autoimmune diseases.

**2. Cancer Therapy:**

* **Anti-Cancer Effects:** 14-OPT exhibits anti-proliferative effects on various cancer cell lines, potentially through inhibiting cell growth, inducing apoptosis, and blocking angiogenesis.
* **Preclinical Studies:** Extensive research is ongoing to investigate its potential as a cancer treatment, focusing on both solid and hematologic malignancies.

**3. Other Potential Applications:**

* **Organ Transplantation:** 14-OPT's immunosuppressive properties make it a potential candidate for preventing rejection after organ transplantation.
* **Inflammatory Diseases:** Its anti-inflammatory effects could be beneficial in treating chronic inflammatory diseases like inflammatory bowel disease.

**Current Research Focus:**

Ongoing research focuses on:

* **Optimizing 14-OPT's delivery methods** to improve its therapeutic effectiveness.
* **Developing new drug formulations** to minimize its side effects.
* **Understanding its precise mechanisms of action** to further explore its therapeutic potential.

**Overall, 14-OPT holds immense promise as a potential treatment for various diseases. Its unique properties and favorable pharmacokinetic profile make it a valuable target for future research and development.**

14-O-phosphonooxymethyltriptolide disodium salt: pro-drug of triptolide; has antineoplastic activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46203139
CHEMBL ID3740500
MeSH IDM0582247

Synonyms (10)

Synonym
minnelide
CHEMBL3740500
trisoxireno(4b,5:6,7:8a,9)phenanthro(1,2-c)furan-1(3h)-one, 3b,4,4a,6,6a,7a,7b,8b,9,10-decahydro-8b-methyl-6a-(1-methylethyl)-6-((phosphonooxy)methoxy)-, sodium salt (1:2), (3bs,4as,5ar,6r,6as,7as,7bs,8as,8bs)-
1254702-87-8
14-o-phosphonooxymethyltriptolide disodium salt
1CIV2UMO40 ,
unii-1civ2umo40
disodium;[(1s,2s,4s,5s,7s,8r,9r,11s,13s)-1-methyl-17-oxo-7-propan-2-yl-3,6,10,16-tetraoxaheptacyclo[11.7.0.02,4.02,9.05,7.09,11.014,18]icos-14(18)-en-8-yl]oxymethyl phosphate
Q27252236
F82363

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" Therefore, this study aimed to investigate whether minnelide, combined with Angptl3 knockout, could completely protect mice with AN and its mechanism."( Minnelide combined with Angptl3 knockout completely protects mice with adriamycin nephropathy via suppression of TGF-β1-Smad2 and p53 pathways.
Ji, B; Liu, J; Ma, Y; Shen, Q; Xu, H; Yin, Y; Yu, J, 2023
)
0.91
" Therefore, the present study aimed to investigate whether minnelide combined with mAb could further protect mice with AN and the underlying mechanisms."( Minnelide combined with anti-ANGPTL3-FLD monoclonal antibody completely protects mice with adriamycin nephropathy by promoting autophagy and inhibiting apoptosis.
Ji, B; Liu, J; Shen, Q; Xu, H; Yin, Y; Yu, J, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (76)

Assay IDTitleYearJournalArticle
AID1265938Toxicity in athymic nude mouse xenografted with human A2780 cells assessed as mortality at 0.6 to 0.9 mg/kg, po administered for 30 days2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265906Stability of the compound in simulated intestinal fluid assessed as compound remaining at pH 7.5 after 8 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265892Chemical stability of the compound in buffer assessed as compound remaining at pH 7.4 after 24 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265937Toxicity in athymic nude mouse xenografted with human A2780 cells assessed as morbidity at 0.6 to 0.9 mg/kg, po administered for 30 days2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265907Stability of the compound in simulated intestinal fluid assessed as compound remaining at pH 7.5 after 24 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265879Chemical stability of the compound in buffer assessed as compound remaining at pH 4 after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265893Chemical stability of the compound in buffer assessed as compound remaining at pH 9 after 1 hr by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265903Stability of the compound in simulated intestinal fluid assessed as compound remaining at pH 7.5 after 1 hr by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265935Prodrug conversion in glycine buffer assessed as bovine intestinal mucosal alkaline phosphatase-mediated triptolide and formaldehyde formation at pH 9.82015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265913Chemical stability of the compound in buffer assessed as pseudo-first-order rate constant at 4 degC at pH 7.4 by Arrhenius plot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265899Stability of the compound in simulated gastric fluid assessed as compound remaining at pH 7.5 after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265902Stability of the compound in simulated gastric fluid assessed as compound remaining at pH 7.5 after 24 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265878Chemical stability of the compound in buffer assessed as compound remaining at pH 4 after 1 hr by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265908Chemical stability of the compound in buffer assessed as pseudo-first-order rate constant at 40 degC at pH 7.4 by Arrhenius plot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265905Stability of the compound in simulated intestinal fluid assessed as compound remaining at pH 7.5 after 4 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265891Chemical stability of the compound in buffer assessed as compound remaining at pH 7.4 after 8 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265897Chemical stability of the compound in buffer assessed as compound remaining at pH 9 after 24 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265923Toxicity in athymic nude mouse xenografted with human HT-29 cells assessed as mortality at 0.9 mg/kg, ip administered for 4 weeks2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265898Stability of the compound in simulated gastric fluid assessed as compound remaining at pH 7.5 after 1 hr by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265904Stability of the compound in simulated intestinal fluid assessed as compound remaining at pH 7.5 after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265924Toxicity in athymic nude mouse xenografted with human HT-29 cells assessed as mortality at 0.9 mg/kg, ip administered for 2 weeks2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265888Chemical stability of the compound in buffer assessed as compound remaining at pH 7.4 after 1 hr by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265926Toxicity in athymic nude mouse xenografted with human HT-29 cells assessed as weight gain at 0.9 mg/kg, ip administered 14 days measured post last dose2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265927Toxicity in athymic nude mouse xenografted with human HT-29 cells assessed as skin irritation at 0.9 mg/kg, ip administered 14 days measured post last dose2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265920Antitumor activity against human HT-29 cells xenografted in athymic nude mouse at 0.3 to 0.9 mg/kg, ip qd administered for 28 days2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265894Chemical stability of the compound in buffer assessed as compound remaining at pH 9 after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265880Chemical stability of the compound in buffer assessed as compound remaining at pH 4 after 4 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265889Chemical stability of the compound in buffer assessed as compound remaining at pH 7.4 after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265882Chemical stability of the compound in buffer assessed as compound remaining at pH 4 after 24 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265874Chemical stability of the compound in buffer assessed as compound remaining at pH 2 after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265869Chemical stability of the compound in buffer assessed as compound remaining at pH 1 after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265925Toxicity in athymic nude mouse xenografted with human HT-29 cells assessed as mortality at 0.9 mg/kg, ip administered for 2 weeks followed by 3 times per week2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265886Chemical stability of the compound in buffer assessed as compound remaining at pH 6 after 8 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265915Half life of the compound in buffer at 4 degC at pH 7.42015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265871Chemical stability of the compound in buffer assessed as compound remaining at pH 1 after 8 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265867Second dissociation constant, pKa2 of the compound by 31P NMR analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265896Chemical stability of the compound in buffer assessed as compound remaining at pH 9 after 8 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265872Chemical stability of the compound in buffer assessed as compound remaining at pH 1 after 24 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265890Chemical stability of the compound in buffer assessed as compound remaining at pH 7.4 after 4 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265868Chemical stability of the compound in buffer assessed as compound remaining at pH 1 after 1 hr by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265881Chemical stability of the compound in buffer assessed as compound remaining at pH 4 after 8 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265901Stability of the compound in simulated gastric fluid assessed as compound remaining at pH 7.5 after 8 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265932Toxicity in athymic nude mouse xenografted with human A2780 cells assessed as moribund condition at 1.2 mg/kg, po administered for 30 days2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265914Half life of the compound in buffer at 25 degC at pH 7.42015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265910Chemical stability of the compound in buffer assessed as pseudo-first-order rate constant at 60 degC at pH 7.4 by Arrhenius plot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265870Chemical stability of the compound in buffer assessed as compound remaining at pH 1 after 4 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265916Shelf life of the compound in buffer assessed as time for 10% loss of compound at 25 degC at pH 7.42015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265873Chemical stability of the compound in buffer assessed as compound remaining at pH 2 after 1 hr by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265900Stability of the compound in simulated gastric fluid assessed as compound remaining at pH 7.5 after 4 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265912Chemical stability of the compound in buffer assessed as pseudo-first-order rate constant at 25 degC at pH 7.4 by Arrhenius plot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1424479Stability assessed as shelf life at 4 degC2017European journal of medicinal chemistry, Dec-15, Volume: 142From bench (laboratory) to bed (hospital/home): How to explore effective natural and synthetic PAK1-blockers/longevity-promoters for cancer therapy.
AID1265929Antitumor activity against human A2780 cells xenografted in athymic nude mouse at 0.6 to 0.9 mg/kg, ip and po administered for 30 days2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265928Toxicity in athymic nude mouse xenografted with human HT-29 cells assessed as necrosis at 0.9 mg/kg, ip administered 14 days measured post last dose2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265922Antitumor activity against human HT-29 cells xenografted in athymic nude mouse at 0.9 mg/kg, ip qd administered for 2 weeks followed by 3 times per week2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265909Chemical stability of the compound in buffer assessed as pseudo-first-order rate constant at 50 degC at pH 7.4 by Arrhenius plot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265887Chemical stability of the compound in buffer assessed as compound remaining at pH 6 after 24 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265919Stability of the compound in glycine buffer at pH 9.8 after 1 hr in absence of bovine intestinal mucosal alkaline phosphatase2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265911Chemical stability of the compound in buffer assessed as pseudo-first-order rate constant at 70 degC at pH 7.4 by Arrhenius plot analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265931Toxicity in athymic nude mouse xenografted with human A2780 cells assessed as dehydration at 1.2 mg/kg, po administered for 30 days2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265917Shelf life of the compound in buffer assessed as time for 10% loss of compound at 4 degC at pH 7.42015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265930Toxicity in athymic nude mouse xenografted with human A2780 cells assessed as anorexia at 1.2 mg/kg, po administered for 30 days2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265884Chemical stability of the compound in buffer assessed as compound remaining at pH 6 after 2 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265883Chemical stability of the compound in buffer assessed as compound remaining at pH 6 after 1 hr by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1555818Half life of the compound2019European journal of medicinal chemistry, Aug-15, Volume: 176Triptolide: Medicinal chemistry, chemical biology and clinical progress.
AID1265895Chemical stability of the compound in buffer assessed as compound remaining at pH 9 after 4 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265885Chemical stability of the compound in buffer assessed as compound remaining at pH 6 after 4 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1555819Aqueous solubility of the compound2019European journal of medicinal chemistry, Aug-15, Volume: 176Triptolide: Medicinal chemistry, chemical biology and clinical progress.
AID1265918Half life of the compound in glycine buffer assessed as bovine intestinal mucosal alkaline phosphatase-mediated compound degradation at pH 9.82015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265933Toxicity in athymic nude mouse xenografted with human A2780 cells assessed as survival at 0.6 to 0.9 mg/kg, ip administered for 30 days2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1424478Solubility of the compound2017European journal of medicinal chemistry, Dec-15, Volume: 142From bench (laboratory) to bed (hospital/home): How to explore effective natural and synthetic PAK1-blockers/longevity-promoters for cancer therapy.
AID1265921Antitumor activity against human HT-29 cells xenografted in athymic nude mouse at 0.9 mg/kg, ip qd administered for 4 weeks2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265877Chemical stability of the compound in buffer assessed as compound remaining at pH 2 after 24 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265876Chemical stability of the compound in buffer assessed as compound remaining at pH 2 after 8 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1265875Chemical stability of the compound in buffer assessed as compound remaining at pH 2 after 4 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
AID1707230Cytotoxicity against human Panc-1 cells incubated for 48 hrs by CCK8 assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1265866Aqueous solubility of the compound in Tris buffer at pH 7.4 at room temperature by HPLC analysis2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (33)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's28 (84.85)24.3611
2020's5 (15.15)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.03

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.03 (24.57)
Research Supply Index3.53 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews5 (15.15%)6.00%
Case Studies1 (3.03%)4.05%
Observational0 (0.00%)0.25%
Other27 (81.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]