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1.
Analyst ; 2021 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-34585179

RESUMO

Most of the ONOO- fluorescent probes have restricted applications because of their aggregation-caused quenching (ACQ) effect, long response time and low fluorescence enhancement. Herein, we developed a novel AIEgen fluorescent probe (PE-XY) based on a benzothiazole and quinolin scaffold with high sensitivity and selectivity for imaging of ONOO-. The results indicated that probe PE-XY exhibited fast response towards ONOO- with 2000-fold enhancement of fluorescence intensity ratio in vitro. Moreover, PE-XY exhibited a relatively high sensitivity (limit of detection: 8.58 nM), rapid response (<50 s), high fluorescence quantum yield (δ = 0.81) and excellent selectivity over other analytes towards ONOO-in vitro. Furthermore, PE-XY was successfully applied to detect endogenous ONOO- levels in living HeLa cells, C. elegans and inflammatory mice with low cytotoxicity. Overall, this work provided a novel fast-response and highly selective AIEgen fluorescent probe for real-time monitoring ONOO- fluctuations in living systems.

2.
Biomater Sci ; 9(19): 6501-6509, 2021 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-34582538

RESUMO

Recently, hypothermal photothermal therapy (HPTT) seemed essential for the future clinical transformation of cancer optical therapies. However, at a lower working temperature, heat shock proteins (HSPs) seriously affect the anti-tumor effect of HPTT. This work reports a reasonable design of a dual-responsive nanoplatform for the synergistic treatment of chemotherapy and HPTT. We adopted a one-step method to wrap indocyanine green (ICG) into imidazole skeleton-8 (ZIF-8) and further loaded it with the chemotherapy drug doxorubicin (DOX). Furthermore, we introduced Hsp-70 siRNA to block the affection of HSPs at an upstream node, thereby avoiding the side effects of traditional heat shock protein inhibitors. The prepared ZIF-8@ICG@DOX@siRNA nanoparticles (ZID-Si NPs) could significantly improve the stability of siRNA to effectively down-regulate the expression of HSP70 protein during the photothermal therapy, thus realizing the pH-controlled and NIR-triggered release of the chemotherapeutical drug DOX. Moreover, tumors were also imaged accurately by ICG wrapped in ZID-Si nanoparticles. After the evaluation of the in vitro and in vivo photothermal effect as well as the anti-tumor activity, we found that the added Hsp-70 siRNA enhanced the synergistic anti-cancer activity of HPTT and chemotherapy. In summary, this work holds great potential in cancer treatment, and suggests better efficacy of synergistic chemo/HPTT than the single-agent therapy.


Assuntos
Hipertermia Induzida , Nanopartículas , Doxorrubicina , Liberação Controlada de Fármacos , Verde de Indocianina , Terapia Fototérmica , RNA Interferente Pequeno/genética
3.
Talanta ; 235: 122796, 2021 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-34517654

RESUMO

Bone metastasis of malignant solid tumors has become one of the most serious complications, especially in breast cancer, which was particularly challenging for early detection and treatment in clinical practice. In this work, we reported a new fluorescently labeled bisphosphonate for bone metastasis detection of breast cancer. The designed probes were based on Rhodamine B and bisphosphonate as recognition group, which can specifically target hydroxyapatite (HA) existed in bone tissue. After the osteoclasts were adsorbed on the bone surface, the surrounding microenvironment was acidified, causing the HA to locally dissolve. The probe bound to the HA was then released, and realized the fluorescence turn on under acidic conditions. In vitro experiments showed that G0 was more excellent than G2 owing to shorter connecting arm. Subsequently, we proved that G0 could combine with HA rapidly and exhibit excellent response in solid state. More importantly, we established a model of bone metastasis with MDA-MB-231 cells which was similar to the clinical cases and evaluated the theranostics value of G0 prospectively, which provide the potential application prospect in clinical.


Assuntos
Neoplasias Ósseas , Neoplasias da Mama , Neoplasias Ósseas/tratamento farmacológico , Osso e Ossos , Neoplasias da Mama/tratamento farmacológico , Difosfonatos , Feminino , Humanos , Osteoclastos , Medicina de Precisão , Microambiente Tumoral
4.
Anal Chim Acta ; 1177: 338786, 2021 Sep 08.
Artigo em Inglês | MEDLINE | ID: mdl-34482889

RESUMO

Biological thiols importantly regulate the intracellular redox activity and metabolic level, but many of the developed probes for biothiols are facing difficulty in effectively distinguishing GSH from Cys/Hcy due to the similarity in mechanism. In this work, despite the previous pattern of "Logic Gate", we reported the concept of "Fluorescence Fusion" for the first time to achieve only one excitation-emission process. The exploited the probe, MZ-NBD, could quickly measure GSH in 10 min with a large Stokes shift (130 nm). Though the reacting mechanism was similar, only GSH could cause the "Fluorescence Fusion" with only one strong fluorescence response while Cys/Hcy caused two peaks. Adjusting the excitation wavelength could hardly split the fused peak into two. Though image recognition by artificial intelligence could easily distinguish the patterns of peaks, here we used the signal-treating method to realize the high selectivity towards GSH. Moreover, MZ-NBD could be utilized for rapid detection of GSH in living MCF-7 cells, which was more suitable for GSH than using the "Logic Gate" strategy. More than introducing a novel probe with the new concept, this work was meaningful as the linker of traditional reaction-based fluorescent probes and potential image recognition by artificial intelligence, thus led to various future researches in inter-disciplines.


Assuntos
Cisteína , Glutationa , Inteligência Artificial , Fluorescência , Corantes Fluorescentes , Glutationa/isolamento & purificação , Homocisteína , Humanos , Células MCF-7
5.
Food Chem ; 371: 131128, 2021 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-34563970

RESUMO

Lithocarpus polystachyus Rehd. known as Sweet Tea in China has attracted lots of interest for its good hypoglycemic effect and the potential as a hypoglycemic agent. Based on affinity separation-UPLC-Q-TOF-MS/MS, 54 potential α-glucosidase inhibitiors were identified and 44 were structurally determined. Out of them, 41 were identified for the first time from this plant including flavonoids, fatty acids, triterpenes, alkaloids, and coumarins. Enzyme assays revealed that flavonoids exhibited higher inhibitory activity against α-glucosidase than others with astilbin (IC50 = 6.14 µg·mL-1), morin (IC50 = 8.46 µg·mL-1), and naringenin (IC50 = 10.03 µg·mL-1) showing 2- to 4-fold higher potency than the positive control acarbose. They were proved as reversible inhibitors with mixed inhibition mechanism. Ki (Ki') values and molecular dockings strongly supported the potency order of astilbin, morin and naringenin that showed in the enzyme assays.

6.
Eur J Med Chem ; 225: 113746, 2021 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-34388382

RESUMO

Theranostic prodrug was highly desirable for precise diagnosis and anti-cancer therapy to decrease side effects. However, it is difficult to conjugate chemo-drug and molecular probe for combined therapy due to the complex pharmacokinetics of different molecules. Here, a novel anticancer theranostic prodrug (BTMP-SS-PTX) had been designed and synthesized by conjugating paclitaxel (PTX) with 2-(benzo[d]thiazol-2-yl)-4-methoxyphenol (BTMP) through a disulphide (-S-S-) linkage, which was redox-sensitive to the high concentration of glutathione in tumors. Upon activation with glutathione in weakly acid media, the BTMP-SS-PTX can be dissociated to release free PTX and visible BTMP, which realized the visual tracking of free drug. The cytotoxicity study demonstrated that soluble prodrug BTMP-SS-PTX displayed more outstanding anticancer activity in HepG2, MCF-7 and HeLa cells, lower toxicity to non-cancer cells (293 T) than free drugs. Furthermore, BTMP-SS-PTX was still able to induce apoptosis of HeLa cells and significantly inhibited tumor growth in HeLa-xenograft mouse model. On the basis of these findings, BTMP-SS-PTX could play a potential role in cancer diagnosis and therapy.

7.
Mini Rev Med Chem ; 2021 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-34353251

RESUMO

Since the outbreak of COVID-19, it has been an epidemic for nearly a year. COVID-19 has brought painful disasters to people all over the world. It not only threatens lives and health, but also induces economic crises. At present, promising methods to eradicate COVID-19 mainly include drugs and vaccines. Enzyme inhibitors have always been a reliable strategy for the treatment of related diseases. Scientists worldwide have worked together to study COVID-19, have obtained the structure of key SARS-CoV-2 associated enzymes, and reported the research of inhibitors of these enzymes. This article summarizes COVID-19-related enzyme inhibitors' recent development, mainly including 3CLpro, PLpro, TMPRSS2, and RdRp inhibitors, hoping to provide valuable weapons in the ensuing battle against COVID-19.

8.
Nanomedicine ; 37: 102440, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34256062

RESUMO

Lately, chemotherapy and photodynamic therapy (PDT) synergistic therapy has become a promising anti-cancer treatment mean. However, the hypoxia in tumor leads to huge impediments to the oxygen-dependent PDT effects. In this work, a multifunctional nanoplatform (TUDMP) based on a multivariable porphyrin-nMOFs core and a manganese dioxide (MnO2) shell was prepared for relieving tumor hypoxia and enhancing chemo-photodynamic synergistic therapy performance. The obtained TUDMP nanoplatform could effectively catalyze the hydrolysis of hydrogen peroxide to generate oxygen and also lead to consumption of antioxidant GSH, thereby facilitating the production of cytotoxic reactive oxygen species (ROS) by photosensitizer under laser irradiation. More importantly, the decomposition of the MnO2 shell would further promote the release of the loaded doxorubicin (DOX), and thus an efficient chemo-PDT synergistic therapy was realized. Both in vitro and in vivo experimental results demonstrated the oxygen self-sufficient multifunctional nanoplatform could exhibit significantly enhanced anticancer efficiencies compared with chemotherapy or PDT alone.

9.
J Mater Chem B ; 9(30): 6068-6075, 2021 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-34286809

RESUMO

Mitochondrial proteins, most of which are encoded in the nucleus and the rest of which are regulated by the mitochondrial genome, play pivotal roles in essential cellular functions. However, fluorescent probes that can be used for monitoring mitochondrial proteins have not yet been widely developed, thereby severely limiting the exploration of the functions of proteins in mitochondria. Towards this end, here we propose a near-infrared (NIR) fluorescence probe MPP to effectively illuminate the dynamic changes in mitochondrial proteins in live cells under oxidative stress, with excellent temporal and spatial resolution. Of particular importance, MPP extends the study of the pharmacology involved in apoptosis induced by anti-cancer drugs (hydroxycamptothecin (HCPT), epirubicin (Epi) and cyclophosphamide (CPA)) for the first time. Furthermore, employing a protein-activatable strategy, this probe could serve as an excellent phototherapeutic agent in photodynamic therapy (PDT). Finally, in vivo experiments suggest that this versatile probe can be used to image tumors in HeLa tumor-bearing mice for 24 h, which demonstrates that our probe could play a dual role as a robust phototherapeutic and imaging agent.

10.
J Mater Chem B ; 9(23): 4678-4689, 2021 06 16.
Artigo em Inglês | MEDLINE | ID: mdl-34075929

RESUMO

In recent years, the antitumor application of photodynamic therapy (PDT) has gained widespread interest in treating solid tumors. Due to the hypoxic environment in tumors, the major limit of PDT seems to be the source of oxygen. In this work, we attempted to relieve hypoxia and enhance photodynamic therapy, and therefore, designed and assembled a catalytic cascade-enhanced PDT multifunctional nanoplatform. The mentioned platform termed UIO@Ca-Pt is based on porphyrinic metal-organic framework (UIO) combination, which is simultaneously loaded by CaO2 NPs with polydopamine (PDA) and then the Pt raw material to further improve biocompatibility and efficiency. In a tumor microenvironment, CaO2 could react with water to generate calcium hydroxide and hydrogen peroxide, which was further decomposed by Pt nanoparticles to form oxygen, thereby facilitating the generation of cytotoxic singlet oxygen by photosensitizer TCPP under laser irradiation. Both in vitro and in vivo experiment results confirmed the excellent oxygen production capacity and enhanced PDT effect of UIO@Ca-Pt. With guaranteed safety in PDT, the oxygen-supplying strategy might stimulate considerable interest in the development of various metal-organic materials with multifunctionality for tumor diagnosis and therapy.


Assuntos
Estruturas Metalorgânicas/química , Fotoquimioterapia/métodos , Porfirinas/química , Animais , Catálise , Linhagem Celular , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Camundongos , Camundongos Endogâmicos BALB C , Análise Multivariada , Microambiente Tumoral/efeitos dos fármacos
11.
Talanta ; 232: 122467, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34074439

RESUMO

Hydrogen polysulfide (H2Sn, n > 1), a member of reactive sulfur species (RSS), is primarily generated during the crosstalk between H2S and reactive oxygen species (ROS), which plays important role in physiological and pathological processes. Ferroptosis is a new non-classical mode of cell death, in which ROS-associated lipid peroxidation and iron-dependent accumulation are the main features. However, the biological effects of H2Sn on ferroptosis and the detailed mechanisms of action remain poorly understood. Thus, there is an urgent need to develop highly selective and sensitive chemical tools for monitoring H2Sn in living cells. Herein, we develop a two-photon fluorescent probe (PSP) for specifically imaging H2Sn in live cells and tumor spheroids. This probe exhibited a sensitive and selective response to H2Sn, which had been used for imaging exogenous and endogenous H2Sn in living cells by confocal imaging and high content imaging. PSP exhibits excellent photo-stability and two-photon imaging performance when irradiating at 880 nm in 3D HeLa multicellular tumor spheroids. Importantly, our studies revealed that H2Sn levels were significantly up-regulated during ferroptosis. These excellent properties ensure that PSP is a promising two-photon probe for exploring the biological and pathological effects of H2Sn during ferroptosis.


Assuntos
Ferroptose , Sulfeto de Hidrogênio , Corantes Fluorescentes , Humanos , Hidrogênio , Sulfetos
12.
Curr Top Med Chem ; 2021 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-33982652

RESUMO

With the rapid development of computer science in scopes of theory, software, and hardware, artificial intelligence (mainly in the form of machine learning and more complex deep learning) combined with advanced cheminformatics is playing an increasingly important role in the drug discovery process. This development has also facilitated privileged scaffold-related research. By definition, a privileged scaffold is a structure that frequently occurs in diverse bioactive molecules. It either has a diverse family affinity or is selective to multiple family members in a superfamily, whilst is different from the "frequent hitters" or the "pan-assay interference compounds". The long history of the use of this concept has witnessed a functional shift from stand-alone technology towards an integrated component in the drug discovery toolbox. Meanwhile, continuing efforts have been dedicated to deepen the understandings of the features of known privileged scaffolds. In this contribution, we focus on the current privileged scaffold-related research driven by state-of-art artificial intelligence approaches and cheminformatics. Representative cases with an emphasis on distinct research aspects are presented, including an update of the knowledge on privileged scaffolds; proof-of-concept tools and workflows to identify privileged scaffolds and to carry on de novo design; informatic SAR models with diversely complex data sets to provide an instructive prediction on new potential molecules bearing privileged scaffolds.

13.
Curr Med Chem ; 2021 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-33797359

RESUMO

Focal Adhesion Kinase (FAK) is a non-receptor tyrosine kinase involved in the process of cell proliferation, survival, migration, and invasion. It has become a promising therapeutic target for treatment of human metastatic cancers due to its overexpression and/or activation in multiple cancer types. Since FAK is emerging as a potential cancer target because of its overexpression at both the transcriptional and translational level in cancer, different types of FAK inhibitors with diversified scaffolds have been discovered in the past few years. In this review, the progress of recently discovered small molecule FAK inhibitors was summarized. Major efforts have been focused on the rational design and synthesis of small molecule FAK inhibitors, and their structure-activity relationship (SAR) analysis were also discussed. Among them, while type I inhibitors remain as the major focuses, type II inhibitors and novel allosteric FAK inhibitors (type III inhibitors) have been developed to improve both potency and selectivity. Meanwhile, novel strategies, such as targeting FAK using inhibitors of protein-protein interactions were also discovered. Lastly, some insights and perspectives on the future development of FAK inhibitors as anticancer therapeutics have been provided.

14.
15.
Mini Rev Med Chem ; 21(14): 1888-1908, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33663367

RESUMO

Virus is a type of noncellular organism, which is simple in structure, small in size and contains only one kind of nucleic acid (RNA or DNA). It must be parasitized in living cells and proliferates by replication. Viruses can infect plants or animals, which leads to many epidemic diseases, such as the current pandemic COVID-19. Viral infectious diseases have brought serious threats to the health of people around the world. Natural products are chemical substances that are usually produced by living organisms and have biological or pharmacological activity. Many of these natural products show antiviral activity. Based on the increasing importance of antiviral research, this paper focuses on the discovery and development of antiviral natural products since 2010.


Assuntos
Antivirais/farmacologia , Produtos Biológicos/farmacologia , COVID-19/tratamento farmacológico , Descoberta de Drogas , SARS-CoV-2 , Animais , Antivirais/química , Produtos Biológicos/química , Humanos , Vírus de Plantas/efeitos dos fármacos
16.
Drug Dev Res ; 2021 Mar 06.
Artigo em Inglês | MEDLINE | ID: mdl-33675542

RESUMO

A series of novel indole-1,2,4-triazole derivatives have been designed, synthesized, and evaluated as potential tubulin polymerization inhibitors. The top hit 12, bearing the 3,4,5-trimethoxyphenyl moiety, exhibited substantial anti-proliferative activity against HepG2, HeLa, MCF-7, and A549 cells in vitro with IC50 values of 0.23 ± 0.08 µM, 0.15 ± 0.18 µM, 0.38 ± 0.12 µM, and 0.30 ± 0.13 µM, respectively. It also inhibited tubulin polymerization with the IC50 value of 2.1 ± 0.12 µM, which was comparable with that of the positive controls. Furthermore, compound 12 regulated the expression of cell cycle-related proteins (Cyclin B1, Cdc25c, and Cdc2) and apoptosis-related proteins (Bcl-2, Bcl-x, and Mcl-1). Mechanistically, compound 12 could arrest cell cycle at the G2/M phase, thus induce an increase of apoptotic cell death. In addition, molecular docking hinted the possible interaction mode of compound 12 into the colchicine binding site of tubulin heterodimers. According to the applications of microtubule-targeting agents in both direct and synergistic cancer therapies, we hope this work might be of significance for future researches.

17.
Anal Chim Acta ; 1152: 338243, 2021 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-33648638

RESUMO

Cysteine (Cys) is an indispensable small organic molecule containing sulfhydryl groups, which has essential regulatory effects on the physiological process of human body. In this work, a red emission fluorescent probe TCFQ-Cys was designed and exploited based on 2-(3-cyano-4,5,5-trimethylfuran-2(5H)-ylidene) malononitrile-derivatives. The probe could effectively monitor Cys through the typical acrylate cleavage. The detecting system showed a red emission at 633 nm and the fluorescence was stable within the pH range of 6-9. The detection could be completed in 30 min. TCFQ-Cys presented high sensitivity with a detection limit of 0.133 µM and high selectivity towards Cys from other biological mercaptans. The most important feature was that the system had a wide linear range of 0-300 µM, which covered the physiological requirements of Cys detection. Subsequently, we conducted the biological imaging of Cys in MCF-7 cells and Caenorhabditis elegans (C. elegans). Therefore, TCFQ-Cys had a practical application prospect for further investigating the physiological function of Cys.


Assuntos
Cisteína , Corantes Fluorescentes , Animais , Caenorhabditis elegans , Células HeLa , Humanos , Compostos de Sulfidrila
18.
Curr Med Chem ; 28(28): 5808-5830, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33530900

RESUMO

BACKGROUND: In the past few decades, with the abuse of antibiotics, bacterial resistance has enhanced constantly. More and more super species of bacteria, which are seriously threatening human health, have been discovered. Developing novel antibacterial agents to overcome the drug-resistance is an urgent duty. We all know that blocking the information-transfer of bacterial DNA and RNA is one of the effective ways to inhibit bacterial growth. Therefore, as the indispensable enzyme for DNA replication and transcription, DNA gyrase is one of the important targets for bacterial inhibitors. Accordingly, many inhibitors of DNA gyrase have also been developed. METHODS: In this review, to highlight the recent progress in DNA gyrase inhibitors, the study in this field over the past three years (2017-2019) was summarized and organized based on their backbones or core moieties. Both of the subunits of DNA gyrase were taken into consideration. RESULTS: These DNA gyrase inhibitors have been classified based on their backbones or core moieties. After the comparison of the divided 14 categories, we could achieve some clues for future modification. In particular, we found that benzodiazepines and naphthalene heterocycles were the most common structures in the drug design. On the other hand, isopropyl and cyclopropyl have also been used in drug design, which provides more inspiration for the investigations. Except for GSK2140944, which has entered the phase III clinical trial stage, other compounds here were not fully promulgated with their optimal pharmacokinetic activity. CONCLUSION: We briefly summed up the current situation and future challenges on this topic. Through the discussion of the design strategies and drug effect, we hope that this review can provide a focused direction for future researches.


Assuntos
DNA Girase , Inibidores da Topoisomerase II , Antibacterianos/farmacologia , Bactérias , DNA Bacteriano , Humanos , Testes de Sensibilidade Microbiana , Inibidores da Topoisomerase II/farmacologia
19.
Int J Biol Macromol ; 175: 451-458, 2021 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-33556404

RESUMO

Enzyme reaction has been accepted widely in numerous applications owing to the high efficiency and stereo-selectivity, as well as simple preparation by gene engineering. However, the fragility and complex purification process of the enzyme are long-standing problems which limit the large-scale application. One possible solution may be the enzyme immobilization. As one type of porous material with high loading capacity and designable functionality, Metal-Organic Frameworks (MOFs) are ideal choices for the immobilization of enzyme with a considerable interest in recent years. In this study, d-amino acid transaminase (DAT), an important enzyme for industrial synthesis of d-Ala, was covalently immobilized on the surface of a star MOFs material, UiO-66-NH2. Interestingly, we found that the nanoscale hybrid enzyme UiO-66-NH2-Gd-DAT not only maintained the high catalytic efficiency but also got rid of the interference of polluting enzymes, which meant that we could obtain efficient and stereo-selective immobilized enzyme without complex purification process. In general, our findings demonstrated that using UiO-66-NH2 might be a promising strategy to immobilize enzyme and produce effective biocatalyst with high activity and stereo-selectivity.


Assuntos
Alanina/biossíntese , Compostos Organometálicos/química , Ácidos Ftálicos/química , Transaminases/química , Adsorção , Aminoácidos , Catálise , Enzimas Imobilizadas/química , Estruturas Metalorgânicas/química , Porosidade , Transaminases/metabolismo , Água , Purificação da Água
20.
Bioorg Chem ; 108: 104585, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-33508676

RESUMO

In this work, a series of diaryl benzo[b][1,4]thiazepine derivatives D1-D36 were synthesized and screened as tubulin polymerization inhibitors with anti-tumor potency. They were designed by introducing the seven-member ring benzothiazepine as the linker for CA-4 modification for the first time. Among them, the hit compound D8 showed potential on inhibiting the growth of several cancer cell lines (IC50 values: 1.48 µM for HeLa, 1.47 µM for MCF-7, 1.52 µM for HT29 and 1.94 µM for A549), being comparable with the positive controls Colchicine and CA-4P. The calculated IC50 value of D8 as an tubulin polymerization inhibitor was 1.20 µM. The results of the flow cytometry assay revealed that D8 could induce the mitotic catastrophe and the death of living cancer cells. D8 also indicated the anti-vascular activity. The possible binding pattern was implied by docking simulation, inferring the possibility of introducing interactions with the nearby tubulin chain. Since the novel structural trial has been conducted with preliminary discussion, this work might stimulate new ideas in further modification of tubulin-related anti-cancer agents and therapeutic approaches.


Assuntos
Antineoplásicos/farmacologia , Tiazepinas/farmacologia , Moduladores de Tubulina/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Polimerização/efeitos dos fármacos , Relação Estrutura-Atividade , Tiazepinas/síntese química , Tiazepinas/química , Tubulina (Proteína)/metabolismo , Moduladores de Tubulina/síntese química , Moduladores de Tubulina/química
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