Comparison of the antitumor activity of DTIC and 1-p-(3,3-dimethyl-1-triazeno) benzoic acid potassium salt on murine transplantable tumors and their hematological toxicity

1984 ◽  
Vol 13 (2) ◽  
Author(s):  
Tina Colombo ◽  
Maurizio D'Incalci
Keyword(s):  
Antitumor Activity ◽  
Benzoic Acid ◽  
Potassium Salt ◽  
Hematological Toxicity ◽  
Transplantable Tumors

ChemInform Abstract: Synthesis and Antitumor Activity of Hydrosoluble Analogs of p-(3,3-Dimethyl-1-triazeno)benzoic Acid Potassium Salt.

ChemInform ◽  
2010 ◽  
Vol 23 (20) ◽  
pp. no-no
Author(s):  
A. VARNAVAS ◽  
C. NISI ◽  
L. LASSIANI ◽  
G. SAVA ◽  
L. PERISSIN ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Benzoic Acid ◽  
Potassium Salt

Chemical composition, antitumor activity, and toxicity of essential oil from the leaves of Lippia microphylla

2015 ◽  
Vol 70 (5-6) ◽  
pp. 129-137 ◽  
Author(s):  
Aline L. Xavier ◽  
João Carlos L.R. Pita ◽  
Monalisa T. Brito ◽  
Déborah R.P. Meireles ◽  
Josean F. Tavares ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Antitumor Activity ◽  
Liver Function ◽  
Essential Oil ◽  
Pharmacological Study ◽  
Hematological Toxicity ◽  
Sarcoma 180 ◽  
Hemolytic Assay ◽  
In Vivo Antitumor Activity

Abstract The chemical composition, antitumor activity and toxicity of the essential oil from Lippia microphylla leaves (OEL) were investigated. The major constituents were thymol (46.5%), carvacrol (31.7%), p-cymene (9%), and γ-terpinene (2.9%). To evaluate the toxicity of OEL in non-tumor cells, the hemolytic assay with Swiss mice erythrocytes was performed. The concentration producing 50% hemolysis (HC50) was 300 μg/mL. Sarcoma 180 tumor growth was inhibited in vivo 38% at 50 mg/kg, and 60% at 100 mg/kg, whereas 5-FU at 50 mg/kg caused 86% inhibition. OEL displays moderate gastrointestinal and hematological toxicity along with causing some alteration in liver function and morphology. However, the changes were considered reversible and negligible in comparison to the effects of several anticancer drugs. In summary, OEL displays in vivo antitumor activity and a moderate toxicity, which suggests further pharmacological study.

scholarly journals The Effect of Polyphenolic Composition BP-C3 on the Efficacy and Hematological Toxicity of Cyclophosphamide in the Chemotherapy of Mice Bearing Soft Tissue Sarcomas Induced by Benzo[a]pyrene

2019 ◽  
Vol 18 ◽  
pp. 153473541983377 ◽  
Author(s):  
Andrey V. Panchenko ◽  
Elena I. Fedoros ◽  
Sergey E. Pigarev ◽  
Mikhail A. Maydin ◽  
Ekaterina A. Gubareva ◽  
...  
Keyword(s):  
Soft Tissue ◽  
Antitumor Activity ◽  
Soft Tissue Sarcomas ◽  
Hematological Toxicity ◽  
Tumor Growth Inhibition ◽  
Male Mice ◽  
Blood Cell Count ◽  
Male And Female ◽  
Female Mice ◽  
Polyphenolic Composition

This study aimed to evaluate the effect of lignin-derived polyphenolic composition BP-C3 on the efficacy and hematological toxicity of cyclophosphamide (CPA). Male and female Swiss-H derived mice bearing benzo[a]pyrene-induced soft tissue sarcomas were treated with CPA 300 mg/kg, BP-C3 75 mg/kg, or a combination. Tumor growth inhibition in male mice treated with CPA, BP-C3, or a combination of CPA and BP-C3 was significant and corresponded to 78%, 45%, and 82%, respectively, on day 21 after CPA administration on day 0. In female mice, tumor growth inhibition was 58%, −11%, and 35% when treated with CPA, BP-C3, or a combination of CPA and BP-C3, respectively. CPA administration resulted in significant hematological toxicity evidenced by a decreased white blood cell count on day 4 (2.43 ± 1.77 × 109/L in male mice and 1.19 ± 0.71 × 109/L in female mice) and anemia development on day 7 (6.55 ± 1.74 × 1012/L in male mice and 5.89 ± 2.24 × 1012/L in female mice). The red blood cell count measured on day 7 in animals treated with the combination of BP-C3 and CPA constituted 7.12 ± 1.17 × 1012/L and 7.36 ± 2.07 × 1012/L for male and female mice, respectively. The results of our study demonstrate the antitumor activity of BP-C3 in male mice bearing soft tissue sarcomas. Neither the antitumor activity nor the hematological toxicity of CPA were significantly influenced by BP-C3. A less pronounced effect of CPA on RBC count is demonstrated when this agent is given jointly with BP-C3.

A phase I study of S-1 administration and a 24-h infusion of cisplatin plus paclitaxel in patients with advanced gastric cancer

2006 ◽  
Vol 24 (18_suppl) ◽  
pp. 4074-4074
Author(s):  
H. Iwase ◽  
M. Shimada ◽  
T. Tsuzuki ◽  
M. Okeya ◽  
K. Kobayashi ◽  
...  
Keyword(s):  
Gastric Cancer ◽  
Antitumor Activity ◽  
Advanced Gastric Cancer ◽  
Dose Level ◽  
Combination Chemotherapy ◽  
Single Agent ◽  
Fixed Dose ◽  
Hematological Toxicity ◽  
Level 3 ◽  
Grade 3

4074 Background: S-1 may have a major role in the treatment of gastric cancer as single agent or as a component of combination chemotherapy in Japan. We previously reported a multicentric phase II study of S-1 combined with a 24-h infusion of cisplatin in patients with advanced gastric cancer. This combination was active, safe and had the possibility of being combined with other anticancer drug. Combination chemotherapy with S-1 and cisplatin plus paclitaxel for advanced gastric cancer might yield a stronger antitumor effect. The objective of this study was to determine the dose-limiting toxicity (DLT), the maximum tolerated dose (MTD), the recommended dose (RD), and the preliminary antitumor activity of S-1 and cisplatin plus paclitaxel for advanced gastric cancer. Methods: Paclitaxel was administered on day 1. A fixed dose of S-1 (70 mg/m2/day) was orally administered for 14 consecutive days from day 1, and a 24-h infusion of a fixed dose of cisplatin (60 mg/m2) was administered on day 14 of every 28-day cycle. Four dose escalation levels of paclitaxcel were studied (120, 140, 160, and 180 mg/m2). The DLT was defined as any of the following: grade 3 neutropenia lasting more than 5 days, grade 4 hematological toxicity, grade 3 non-hematological toxicity, or treatment delay of greater than 2 weeks as a result of toxicity. Results: Twenty patients were enrolled. Hematological and non- hematological toxicity of over grade 2 was not observed at dose level 1 and 2. Three patients started at dose level 3. One developed grade 3 neutropenia for 5 days following by grade 2 neutropenia lasted more than 10 days. Five more patients were added at this level. The treatment was delayed over 2 weeks in 1 out of 8 patients. Three patients started at dose level 4. One developed grade 3 neutropenia and needed longer than 14 days to recover. Three patients added this level. In total, at dose level 4 the treatment was delayed over 2 weeks in 3 out of 6 patients as a result of neutropenia. We considered level 4 is the MTD and the RD of paclitaxcel was 160 mg/m2 (dose level 3). The overall response rate was 75%. Conclusions: Triple combination chemotherapy consisting of S-1, cisplatin, and paclitaxel showed a tolerable dose of adverse reactions and favorable antitumor activity for gastric cancer. No significant financial relationships to disclose.

Antitumor acridines with diaminoalkylo pharmacophoric group

2001 ◽  
Vol 73 (9) ◽  
pp. 1421-1428 ◽  
Author(s):  
Jerzy Konopa
Keyword(s):  
Clinical Trials ◽  
Biological Activity ◽  
Antitumor Activity ◽  
Clinical Evaluation ◽  
Wide Spectrum ◽  
Aromatic Rings ◽  
Transplantable Tumors

The substitution of acridine molecule in positions 1 and/or 4 with diaminoalkylo residue may result in obtaining derivatives displaying antitumor activity. The diaminoalkylo residue can be attached to acridine either directly or indirectly as a carboxamido moiety. In the former case, the presence of appropriate substituent in position para to diaminoalkylo residue is crucial for antitumor activity. Also, heterocyclic aromatic rings condensed with the acridine core can be considered as such substituents. Additional substituents introduced into the acridine core, especially those that may be transformed into quinoid systems, significantly increase antitumor activity of modified analogs. It is, however, of utmost importance that the presence of diaminoalkylo residue is the indispensable prerequisite for biological activity of acridines. Among several groups of synthesized diaminoalkyloacridines, the most potent antineoplastic properties toward a wide spectrum of transplantable tumors are exhibited by acridine-4-carboxamides, imidazo-, triazolo-, and pyrazoloacridinones. Two derivatives belonging to the above groups, acridine-4-carboxamide DACA and imidazoacridinone C-1311, are currently in clinical trials. Other derivatives exhibiting potent antitumor activity, that could be considered as close analogs of diaminolkyloacridines, are pyrazoloacridines, one of which is currently under clinical evaluation.

Mutagenic activity of the dacarbazine analog p-(3,3-dimethyl-l-triazeno)benzoic acid potassium salt in bacterial cells

1986 ◽  
Vol 18 (5) ◽  
pp. 491-501 ◽  
Author(s):  
Marisa Tamaro ◽  
Lucilla Dolzani ◽  
Carlo Monti-bragadin ◽  
Gianni Sava
Keyword(s):  
Benzoic Acid ◽  
Potassium Salt ◽  
Mutagenic Activity ◽  
Bacterial Cells

Synthesis and Characterization of New Dibenzo[b, e]Thiepine Derivatives. I

2009 ◽  
Vol 59 (12) ◽  
Author(s):  
Camelia Elena Stecoza ◽  
Miron Teodor Caproiu ◽  
Constantin Draghici ◽  
Corina Ilie ◽  
Ileana Cornelia Chirita
Keyword(s):  
Hydrogen Peroxide ◽  
Spectral Analysis ◽  
Benzoic Acid ◽  
Potassium Salt ◽  
Polyphosphoric Acid ◽  
Chemical Characterization ◽  
Synthesis And Characterization ◽  
Acid Chlorides ◽  
New Compounds

The aim of the present paper was the synthesis and chemical characterization of some original compounds with dibenzo[b,e]thiepine structure. The synthesis of the new compounds was performed in several stages. Thus, by reaction of phtalide with thiophenol potassium salt, we obtained the 2-phenylthiomethyl-benzoic acid. The acid was cyclized with polyphosphoric acid to the desired 6,11-dihydrodibenzo[b,e]thiepin-11(6H)-one, converted afterwards to the corresponding oxime and subsequently to the O-acyloximino-dibenzo[b,e]thiepins by acylation with various substituted benzoic acid chlorides. The oxidation of O-acyloximino-dibenzo[b,e]thiepins with hydrogen peroxide afforded the corresponding sulfones. The new compounds, four O-acyl-oximino-dibenzo[b,e]thiepins, and four O-acyl-oximino-dibenzo[b,e]thiepin-5,5-dioxides, have been characterized by their physical constants (melting point, solubility) and their structures and purity were confirmed by elemental analysis, and spectral analysis (IR, 1H-NMR, 13C-NMR).

THE EFFECTS OF THE COMBINATION OF RAPAMYCIN WITH DOXORUBICIN AND PACLITAXEL ON THE MODELS OF TRANSPLANTABLE TUMORS IN MICE

2019 ◽  
Vol 65 (4) ◽  
pp. 614-622
Author(s):  
Mariya Yurova ◽  
Margarita Tyndyk ◽  
Yekaterina Gubareva ◽  
Yelena Fedoros ◽  
Viktor Anisimov
Keyword(s):  
Antitumor Activity ◽  
Protective Effect ◽  
Total Dose ◽  
Mtor Inhibitor ◽  
Combined Treatment ◽  
Mammary Adenocarcinoma ◽  
Ehrlich Carcinoma ◽  
Tumor Growth Inhibition ◽  
Chemotherapeutic Drugs ◽  
Transplantable Tumors

The study aimed to assess combined treatment with mTOR inhibitor rapamycin and cytotoxic drugs (doxorubicin and paclitaxel) on two models of transplantable tumors - mammary adenocarcinoma in male HER-2/neu transgenic FVB/N mice and solid Ehrlich carcinoma in male 129/Sv mice. Rapamycin (total dose of 3.6 mg kg), doxorubicin (total dose of 15 mg/ kg), paclitaxel (total dose of 6 mg/kg) or their combination were intraperitoneally injected to mice with developed tumor node. Rapamycin showed its own antitumor activity by tumor growth inhibition up to 42% in mammary adenocarcinoma model and up to 57% in Ehrlich carcinoma model. A tendency to an increase in the antitumor activity of chemotherapeutic drugs with the addition of rapamycin was revealed. The cyto-protective effect of the mTOR inhibitor was observed during therapy with doxorubicin and paclitaxel, expressed in a significant decrease in the level of apoptosis in normal epithelium of jejunum crypts. Thus, revealed protective effect of mTOR inhibitor on jejunum epithelium could be applied for reduction of chemotherapeutic drugs enterotoxic effect without any efficiency reduction. Thus, in perspective that could expand the possibilities of standard chemotherapeutic treatment and improve the quality of life of cancer patients.

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