Synthesis and anti-cancer activity of benzothiazole containing phthalimide on human carcinoma cell lines

Kok, Stanton Hon Lung; Gambari, Roberto; Chui, Chung Hin; Yuen, Marcus Chun Wah; Lin, Eva; Wong, Raymond; Lau, Fung Yi; Cheng, Gregory Yin Ming; Lam, William W. Y.; Chan, Sau Hing; Lam, Kim Hung; Cheng, Chor Hing; Lai, Paul B.S.; Yu, Michael Wing Yiu; Cheung, Filly; Tang, Johnny; Chan, Albert S. C.

doi:10.1016/j.bmc.2008.02.005

Cited by 195 publications

(61 citation statements)

References 14 publications

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“…The mechanisms of 1,3-thiazole derivatives antitumor activity may be associated with DNA intercalation [11,12], PRL-3, SHP-2 and JSP-1 inhibition [13][14][15][16], tumor necrosis factor (TNFα) [17], anti-apoptotic bio-complex Bcl-XL-BH3 [18], integrin avb3 [19], others. Thiazole ring belongs to the privileged scaffolds in modern medicinal chemistry [11,20,21], particularly at discovering new anticancer agents.…”

Section: Introductionmentioning

confidence: 99%

Antineoplastic activity of novel thiazole derivatives

Finiuk¹,

Hreniuh²,

Ostapiuk³

et al. 2017

Biopolym. Cell

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The development of novel efficient substances for anticancer chemotherapy is an important problem of medicinal chemistry. Aim. To evaluate the level of cytotoxic action of novel thiazole derivatives towards tumor cell lines of different origin. Methods. Four N acylated 2-amino-5-benzyl-1,3-thiazoles (5a-d) were synthesized by reaction of 2-amino-5-R-benzyl-1,3-thiazoles with acid chlorides in the presence of triethylamine in the dioxane medium. Anticancer screening of the synthesized thiazoles was performed by the MTT assay. Results. Thiazole derivatives were shown to exert antineoplastic activity towards different types of tumor cells. The anti-glioma and anti-melanoma selectivity of these derivatives action was demonstrated. The compound 5a was found to be the most toxic for human glioblastoma U251 cells and human melanoma WM793 cells. At the same time, the created compounds possessed low toxicity towards pseudo-normal cells. Conclusion. The novel thiazole derivative 5a was the most toxic against human glioblastoma and melanoma cells. K e y w o r d s: thiazole derivatives, 2-amino-5-benzyl-1,3-thiazoles, anticancer activity, leukemia, glioblastoma, melanoma.

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Section: Introductionmentioning

confidence: 99%

Antineoplastic activity of novel thiazole derivatives

Finiuk¹,

Hreniuh²,

Ostapiuk³

et al. 2017

Biopolym. Cell

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show abstract

“…It was observed that these microcapsules exerted no significant toxicological effect on those human cells at a maximum concentration of 100 μg/ml after 48 h of incubation as shown in Fig. 9A-F, respectively (33)(34)(35)(36)(37)(38). The gelatin microcapsules containing vitamin C were therefore proved to be non-cytotoxic to human cells under in vitro condition.…”

Section: A B Cmentioning

confidence: 86%

Cosmetic textiles with biological benefits: Gelatin microcapsules containing Vitamin C

et al. 2009

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Abstract. In recent years, textile materials with special applications in the cosmetic field have been developed. A new sector of cosmetic textiles is opened up and several cosmetic textile products are currently available in the market. Microencapsulation technology is an effective technique to control the release properties of active ingredients that prolong the functionality of cosmetic textiles. This study discusses the development of cosmetic textiles and addresses microencapsulation technology with respect to its historical background, significant advantages, microencapsulation methods and recent applications in the textile industry. Gelatin microcapsules containing vitamin C were prepared using emulsion hardening technique. Both the optical microscopy and scanning electron microscopy demonstrated that the newly developed microcapsules were in the form of core-shell spheres with relatively smooth surface. The particle size of microcapsules ranged from 5.0 to 44.1 μm with the average particle size being 24.6 μm. The gelatin microcapsules were proved to be non-cytotoxic based on the research findings of the toxicity studies conducted on human liver and breast cell lines as well as primary bone marrow culture obtained from patient with non-malignant haematological disorder. The gelatin microcapsules were successfully grafted into textile materials for the development of cosmetic textiles.

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“…Benzothiazole derivatives have been known for diverse biological functions, including antitubercular, antimalarial, antihelmintic, analgesic, anticonvulsant, anti-inflammatory and antitumor activities (12,13). 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).…”

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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Synthesis and anti-cancer activity of benzothiazole containing phthalimide on human carcinoma cell lines

Cited by 195 publications

References 14 publications

Antineoplastic activity of novel thiazole derivatives

Antineoplastic activity of novel thiazole derivatives

Cosmetic textiles with biological benefits: Gelatin microcapsules containing Vitamin C

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

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