Synthesis, in vitro and in vivo cytotoxicity, and prediction of the intestinal absorption of substituted 2-ethoxycarbonyl-imidazo[2,1-b]benzothiazoles

Trapani, Giuseppe; Franco, Massimo; Latrofa, Andrea; Reho, A.; Liso, Gaetano

doi:10.1016/s0928-0987(01)00173-7

Cited by 71 publications

(39 citation statements)

References 20 publications

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“…The benzothiazole moiety modified with certain functional groups, such as imidazole and aryl, can significantly inhibit the growth of certain cancer cell lines (14)(15)(16). However, the majority of studies focused on designing new benzothiazole compounds by substituting 2-aminobenzothiazoles or 2-arylbenzothiazoles; only a few investigators employed the benzothiazole-2-thiol as a functional group.…”

Section: Discussionmentioning

confidence: 99%

A novel inhibitor of Rho GDP-dissociation inhibitor α improves the therapeutic efficacy of paclitaxel in Lewis lung carcinoma

et al. 2015

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Abstract. Molecular-targeted therapies are considered a promising strategy for the treatment of most types of human cancer. Rho GDP-dissociation inhibitor α (RhoGDIα), which functions mainly by controlling the cellular distribution and activity of Rho GTPases and is associated with tumor progression and poor prognosis of cancer patients, has become a new promising target for anticancer treatment. Recently, a specific RhoGDIα inhibitor (no. SKLB-163) was developed via computer-aided drug design and de novo synthesis. Previous studies have shown that SKLB-163 had extremely good antitumor activities against diverse cancer cell lines. In the present study, SKLB-163 was used in combination with paclitaxel in order to determine the synergistic effect of the antitumor activity. The findings showed that the combination therapy clearly inhibited cell proliferation and induced apoptosis of LL/2 in vitro. The LL/2 mice model also showed that the combination therapy inhibited tumor growth in vivo. Proliferative cell nuclear antigen (PCNA) immunohistochmeistry and terminal deoxynucleotidyl transferase dUTP nick end-labeling showed that combination therapy inhibited cell proliferation and increased apoptosis compared to the treatment with SKLB-163 or paclitaxel alone. The data suggests that the combination therapy exerted synergistic antitumor effects, providing a novel way to augment the antitumor efficacy of cytotoxic chemotherapy.

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Section: Discussionmentioning

confidence: 99%

A novel inhibitor of Rho GDP-dissociation inhibitor α improves the therapeutic efficacy of paclitaxel in Lewis lung carcinoma

et al. 2015

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“…Benzothiazole derivatives such as, pyrimido benzothiazole, [35] quinoline derivatives, [36] imidazo benzothiazoles, [37] and polymerized benzothiazoles [38] showed potent antitumor activities. In the previous studies benzothiazoles were reported as potent antitumor and antiviral agents [31].…”

Section: Influence Of Synthesized Inhibitors On Activity Of Hnppsmentioning

confidence: 99%

Identification of Potent and Selective Human Ecto-Nucleotide Pyrophosphatase/ Phosphodiesterase-3 (hNPP3) Inhibitors

Iqbal¹

2011

TOEIJ

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NPP3 inhibitors are promising therapeutic agents due to their potential as anti-cancer, anti-metastatic and anti-neurodegenerative drugs. We have identified the first potent and selective inhibitors of human NPP3. We have also estimated the biochemical properties of the main NPP family members that can hydrolyse nucleotides using p-nitrophenyl-5'-thymidine monophosphate as substrate. K m values were found to be 20 ± 4 and 15 ± 6 M for human NPP1 and NPP3, respectively. Maximum velocity (V max ) values calculated for NPP1 and NPP3 were 12 ± 2 and 5 ± 1 nmol p-nitrophenol released/min/mg of crude protein, respectively. A series of benzothiazole derivatives and a series of 1,3,4-oxadiazole-2-thiones was tested on hNPP1 and hNPP3. Benzothiazoles were the most potent non competitive inhibitors of hNPP3 described to date. 1,3,4-oxadiazole-2-thiones were also identified as compounds which inhibited specifically NPP3 over NPP1. The most potent compound was further characterized and found to exhibit a non competitive mechanism of inhibition.

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“…A literature survey performed for the current study revealed that 6-substituted-2-aminobenzothiazole derivatives such as 6-methyl, 6-methoxy, 6-ethoxy and 6-isopropoxy show antibacterial, anti-inflammatory and analgesic properties [9]. Various other derivatives are found to be cytotoxic against various tumors [10,11].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

et al. 2016

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Abstract:A new series of N-(6-arylbenzo [d]thiazol-2-yl)acetamides were synthesized by C-C coupling methodology in the presence of Pd(0) using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolyl)benzo[d]thiazol-2-yl)acetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition.

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Synthesis, in vitro and in vivo cytotoxicity, and prediction of the intestinal absorption of substituted 2-ethoxycarbonyl-imidazo[2,1-b]benzothiazoles

Cited by 71 publications

References 20 publications

A novel inhibitor of Rho GDP-dissociation inhibitor α improves the therapeutic efficacy of paclitaxel in Lewis lung carcinoma

A novel inhibitor of Rho GDP-dissociation inhibitor α improves the therapeutic efficacy of paclitaxel in Lewis lung carcinoma

Identification of Potent and Selective Human Ecto-Nucleotide Pyrophosphatase/ Phosphodiesterase-3 (hNPP3) Inhibitors

Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

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