scholarly journals Encapsulation of Chemotherapeutic Drug Melphalan in Cucurbit[7]uril: Effects on Its Alkylating Activity, Hydrolysis, and Cytotoxicity

ACS Omega ◽  
2018 ◽  
Vol 3 (7) ◽  
pp. 8337-8343 ◽  
Author(s):  
Gustavo Villarroel-Lecourt ◽  
Javiera Carrasco-Carvajal ◽  
Felipe Andrade-Villalobos ◽  
Fresia Solís-Egaña ◽  
Ignacio Merino-San Martín ◽  
...  
Keyword(s):  
Chemotherapeutic Drug ◽  
Alkylating Activity

Alkylating activity of polyphosphate ester in the course of the synthesis of benzimidazoles

1985 ◽  
Vol 50 (9) ◽  
pp. 1959-1961 ◽  
Author(s):  
Giovanni Allunni Bistocchi ◽  
Giovanni De Meo ◽  
Mauro Pedini ◽  
Adolfo Ricci ◽  
Pierre Jacquignon
Keyword(s):  
Furoic Acid ◽  
Alkylating Activity

5-Fluoro-2-(5-nitrofuryl)benzimidazole (I) was synthesized from 4-fluoro-1,2-diaminobenzene and 5-nitro-2-furoic acid using ethyl polyphosphate as cyclization reagent. N-Ethyl derivative was isolated as by-product in substantial amount.

scholarly journals Synergistic effect of tumor chemo-immunotherapy induced by leukocyte-hitchhiking thermal-sensitive micelles

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Jing Qi ◽  
Feiyang Jin ◽  
Yuchan You ◽  
Yan Du ◽  
Di Liu ◽  
...  
Keyword(s):  
Microwave Irradiation ◽  
Antitumor Immunity ◽  
Chemotherapeutic Drugs ◽  
Chemotherapeutic Drug ◽  
A2a Adenosine Receptor ◽  
Adenosine Receptor Antagonist ◽  
Tumor Immunosuppression ◽  
Tumor Immunogenicity ◽  
Sch 58261 ◽  
Tumor Accumulation

AbstractSome specific chemotherapeutic drugs are able to enhance tumor immunogenicity and facilitate antitumor immunity by inducing immunogenic cell death (ICD). However, tumor immunosuppression induced by the adenosine pathway hampers this effect. In this study, E-selectin-modified thermal-sensitive micelles are designed to co-deliver a chemotherapeutic drug (doxorubicin, DOX) and an A2A adenosine receptor antagonist (SCH 58261), which simultaneously exhibit chemo-immunotherapeutic effects when applied with microwave irradiation. After intravenous injection, the fabricated micelles effectively adhere to the surface of leukocytes in peripheral blood mediated by E-selectin, and thereby hitchhiking with leukocytes to achieve a higher accumulation at the tumor site. Further, local microwave irradiation is applied to induce hyperthermia and accelerates the release rate of drugs from micelles. Rapidly released DOX induces tumor ICD and elicits tumor-specific immunity, while SCH 58261 alleviates immunosuppression caused by the adenosine pathway, further enhancing DOX-induced antitumor immunity. In conclusion, this study presents a strategy to increase the tumor accumulation of drugs by hitchhiking with leukocytes, and the synergistic strategy of chemo-immunotherapy not only effectively arrested primary tumor growth, but also exhibited superior effects in terms of antimetastasis, antirecurrence and antirechallenge.

Gold–Nickel Nanowires as Nanomotors for Cancer Marker Biodetection and Chemotherapeutic Drug Delivery

2021 ◽  
Vol 4 (4) ◽  
pp. 3377-3388
Author(s):  
Gozde Yurdabak Karaca ◽  
Filiz Kuralay ◽  
Emre Uygun ◽  
Kadir Ozaltin ◽  
Sezin Eren Demirbuken ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Chemotherapeutic Drug ◽  
Cancer Marker ◽  
Nickel Nanowires

scholarly journals Combinatorial Therapeutic Effect of Inhibitors of Aldehyde Dehydrogenase and Mitochondrial Complex I, and the Chemotherapeutic Drug, Temozolomide against Glioblastoma Tumorspheres

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 282
Author(s):  
Hun Ho Park ◽  
Junseong Park ◽  
Hye Joung Cho ◽  
Jin-Kyoung Shim ◽  
Ju Hyung Moon ◽  
...  
Keyword(s):  
Aldehyde Dehydrogenase ◽  
Cell Metabolism ◽  
Dual Therapy ◽  
Mechanisms Of Action ◽  
Therapeutic Effects ◽  
Chemotherapeutic Drug ◽  
Mitochondrial Complex ◽  
Dual Inhibitors ◽  
Dual Inhibition ◽  
Tumor Bioenergetics

Resident cancer cells with stem cell-like features induce drug tolerance, facilitating survival of glioblastoma (GBM). We previously showed that strategies targeting tumor bioenergetics present a novel emerging avenue for treatment of GBM. The objective of this study was to enhance the therapeutic effects of dual inhibition of tumor bioenergetics by combination of gossypol, an aldehyde dehydrogenase inhibitor, and phenformin, a biguanide compound that depletes oxidative phosphorylation, with the chemotherapeutic drug, temozolomide (TMZ), to block proliferation, stemness, and invasiveness of GBM tumorspheres (TSs). Combination therapy with gossypol, phenformin, and TMZ induced a significant reduction in ATP levels, cell viability, stemness, and invasiveness compared to TMZ monotherapy and dual therapy with gossypol and phenformin. Analysis of differentially expressed genes revealed up-regulation of genes involved in programmed cell death, autophagy, and protein metabolism and down-regulation of those associated with cell metabolism, cycle, and adhesion. Combination of TMZ with dual inhibitors of tumor bioenergetics may, therefore, present an effective strategy against GBM by enhancing therapeutic effects through multiple mechanisms of action.

scholarly journals Podophyllotoxin: History, Recent Advances and Future Prospects

Biomolecules ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 603
Author(s):  
Zinnia Shah ◽  
Umar Farooq Gohar ◽  
Iffat Jamshed ◽  
Aamir Mushtaq ◽  
Hamid Mukhtar ◽  
...  
Keyword(s):  
Structure Optimization ◽  
Cytokine Storm ◽  
Chemotherapeutic Drug ◽  
Future Prospects ◽  
Naturally Occurring ◽  
Pharmacologically Active ◽  
Almost All ◽  
Pharmacologically Active Compounds ◽  
Synthetic Derivatives ◽  
Related Compounds

Podophyllotoxin, along with its various derivatives and congeners are widely recognized as broad-spectrum pharmacologically active compounds. Etoposide, for instance, is the frontline chemotherapeutic drug used against various cancers due to its superior anticancer activity. It has recently been redeveloped for the purpose of treating cytokine storm in COVID-19 patients. Podophyllotoxin and its naturally occurring congeners have low bioavailability and almost all these initially discovered compounds cause systemic toxicity and development of drug resistance. Moreover, the production of synthetic derivatives that could suffice for the clinical limitations of these naturally occurring compounds is not economically feasible. These challenges demanded continuous devotions towards improving the druggability of these drugs and continue to seek structure-optimization strategies. The discovery of renewable sources including microbial origin for podophyllotoxin is another possible approach. This review focuses on the exigency of innovation and research required in the global R&D and pharmaceutical industry for podophyllotoxin and related compounds based on recent scientific findings and market predictions.

Sodium alginate-functionalized nanodiamonds as sustained chemotherapeutic drug-release vectors

Carbon ◽  
2016 ◽  
Vol 97 ◽  
pp. 78-86 ◽  
Author(s):  
Zhifen Cui ◽  
Yu Zhang ◽  
Jichao Zhang ◽  
Huating Kong ◽  
Xiaoxing Tang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Chemotherapeutic Drug
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