bluuebunny/crossref_metadata_2025_split huggingface dataset:
Pyrimidine-fused Dinitrogenous Penta-heterocycles as a Privileged Scaffold
for Anti-Cancer Drug Discovery
Authors: Li Wen , Zhang Jinyang , Wang Min , Dong Ru , Zhou Xin , Zheng Xin , Sun Liping 
Published: January 2022

Abstract:
Pyrimidine-fused derivatives that are the inextricable part of DNA and RNA play a key role in the normal life cycle of cells. Pyrimidine-fused dinitrogenous penta-heterocycles, including pyrazolopyrimidines and imidazopyrimidines are a special class of pyrimidine-fused compounds contributing to an important portion in anti-cancer drug discovery, which has been discovered as the core structure for promising anti-cancer agents used in the clinic or clinical evaluations. Pyrimidine-fused dinitrogenous penta-heterocycles have become one privileged scaffold for anti-cancer drug discovery. This review consists of the recent progress of pyrimidine-fused dinitrogenous penta-heterocycles as anti-cancer agents and their synthetic strategies. In addition, this review also summa-rizes some key structure-activity relationships (SARs) of pyrimidine-fused dinitrogenous penta-heterocycle derivatives as anti-cancer agents.
First Total Synthesis of Isopsoralenoside
Authors: Wu Min , Xu Lijia , Song Mingwei , Li Ying , Wang Yingying , Dong Hongbo 
Published: January 2022

Abstract:
The first total synthesis of the natural product iopsoralenoside, isolated from the n-butyl
alcohol extract of Fructus Psoraleae (FP), was achieved in 17% yield over 7 steps. The key steps of
the process were glycosylation and irradiation promoted by ultraviolet light. This synthesis provided
a sufficient amount of synthesized trans- and cis-isopsoralenoside for further bioassays.
Microwave Irradiated Synthesis of Pyrimidine Containing, Thiazolidin-4-
ones: Antimicrobial, Anti-Tuberculosis, Antimalarial and Anti-Protozoa
Evaluation
Authors: Soni Hetal I. , Patel Navin B. , Parmar Rahul B. , Chan-Bacab Manuel J. , Rivera Gildardo 
Published: January 2022

Aim:
This study aims to synthesize thiazolidine-4-one compounds with a pyrimidine
nucleus and evaluate against different species of bacteria, fungi, protozoa, and the malaria parasite.

Background:
Microwave irradiation was the best method for synthesizing the thiazolidin-4-one
ring system. It took only 15 minutes for synthesizing thiazolidin-4-one while the conventional
method required 12 hours. The rapid reaction was the main concern of this research.

Objective:
Pyrimidine and Thiazolidin-4-one nucleus have broad-spectrum biological activity and
when it is introduced with other hetero atoms containing moiety, many types of biological activities
have been found; antimicrobial, anti-tuberculosis, anti-protozoa, antimalarial are the main activities.
The activity of these compounds inspired us to do extra research on Thiazolidin-4-one fused pyrimidines
with different functional groups. The aim of this study is to synthesize a combination of these
two ring systems in less time by using a microwave irradiation method and to evaluate new
compounds for different bioactivity.

Method:
2-(4-Chlorophenyl)-3-(4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl) thiazolidin-
4-ones (6A-J) were synthesized by microwave irradiation to save energy and time. The structure
of all newly synthesized motifs was characterized by spectral analysis (1H NMR, 13C NMR, IR,
spectroscopy) and screened for antibacterial activity against Escherichia coli, Pseudomonas aeruginosa,
Staphylococcus aureus, and Streptococcus pyogenes, antifungal activity against Candida
albicans, Aspergillus niger, Aspergillus clavatus, anti-tuberculosis activity against M. tuberculosis
H37RV, antimalarial activity against Plasmodium falciparum and anti-protozoa activity against L.
mexicana and T. cruzi.

Result:
Because of microwave irradiation synthesis, time period is very less for preparing the new
compound. Biological response given by compounds 6B, 6C, 6D, 6E, 6G, 6H, and 6J was found excellent.

Conclusion:
Good yield with purity of the newly synthesized thiazolidine-4-one compounds obtained
in less time by using microwave irradiation. The biological response of some of the compounds
of this series was found excellent.
Green Synthesis of 2-thioxothiazolidin-4-one Derivatives in Deep Eutectic
Solvents via Knoevenagel Condensation
Authors: Lončarić Melita , Molnar Maja 
Published: January 2022

Abstract:
Recently, more and more researchers are resorting to green methods and techniques to avoid
environmental pollution. Accordingly, many researchers have been working on the development of
new green synthetic procedures trying to avoid the use of toxic organic solvents. A sustainable concept
of green and environmentally friendly solvents in chemical synthesis nowadays encompasses a
relatively new generation of solvents called deep eutectic solvents (DESs). DESs often have a dual role
in the synthesis, acting as both solvents and catalysts. In this study, DESs are used in the Knoevenagel
synthesis of rhodanine derivatives, with no addition of conventional catalysts. A model reaction of
rhodanine and salicylaldehyde was performed in 20 different DESs at 80°C, in order to find the best
solvent, which was further used for the synthesis of the series of desired compounds. A series of
rhodanines was synthesized in choline chloride: acetamide (ChCl:acetamide) DES with good to
excellent yields (51.4-99.7%).
Estrogen Receptor Beta (ERβ) Expression in Different Subtypes of Malignant
Pleural Mesothelioma
Authors: Shamaei Masoud , Pourabdollah Mihan , Pourdowlat Guitti , Parvizi Maryam , Boyadjian Shogher 
Published: January 2022

Background:
Estrogen receptor beta (ERβ) is a potential target for cancer therapy as a
tumor suppressor. Malignant pleural mesothelioma (MPM) is a rare but fatal cancer. This study
tries to estimate the incidence of ERβ expression in the various subtypes of MPM tumors.

Methods and Materials:
In a retrospective study performed at a pulmonary tertiary referral hospital,
formalin-fixed paraffin-embedded human tissues of 46 definitive MPM were evaluated for expression
of ERβ by immunohistochemistry.

Results:
ERβ was detected in 14 cases (30.4%) out of the total 46 patients with a mean age of
58.08±11.59 SD, including 33 (71.7%) males. There was no statistically significant difference in
patients with positive ERβ staining versus negative cases in age and sex (P >0.05). MPM subtypes
included 36 (78.2%) cases of epithelioid mesothelioma, 3 (6.5%) cases of sarcomatoid, 5 (10.8%)
cases of biphasic, and 2 (4.3%) cases of desmoplastic subtype. ERβ expression was observed only
in epithelioid (11 of total 36 cases) and biphasic (3 of total 5 cases) tumors. There was no significant
difference in the incidence of ERβ expression in different subtypes of malignant pleural mesothelioma.
Statistical analysis shows a significant difference in the expression of ERβ in the
epithelioid subtype (with a more favorable prognosis) versus non-epithelioid subtypes (with poor
prognosis, including sarcomatoid, desmoplastic, and biphasic) (P = 0.024).

Discussion and Conclusion:
Considering the higher proportion of the epithelioid type of MPM
with ERβ expression, this highlights the role of ERβ in target therapy of MPM tumor, especially in
the epithelioid subtype with a more favorable prognosis. A better understanding of the pathology
of mesothelioma will eventually contribute to the development of therapies beyond the existing
therapeutic platform
Correlation Analysis of Surgical Efficacy and Risk Factors of Cervical
Spondylotic Myelopathy with High Signal Intensity on MRI-T2WI
Authors: Xu Hongguang , Xu Ziang , Xiao Liang , Liu Chen , Zhao Quanlai , Zhang Yu 
Published: January 2022

Objectives:
The purpose of this study was to investigate the surgical efficacy and risk
factors of cervical spondylotic myelopathy (CSM) patients with increased signal intensity (ISI) on
T2-weighted magnetic resonance imaging (MRI-T2WI).

Methods:
We compared the surgical outcomes of CSM patients with and without ISI. In addition,
we compared the efficacy of anterior and posterior cervical decompression in CSM patients with
ISI. We also analyzed the risk factors of MRI-T2WI ISI in CSM patients.

Results:
The incidence of ISI among 153 CSM patients was 71.89 %. The JOA score and JOA remission
rate were better in the ISI-free than in the ISI group. The postoperative JOA score and
JOA remission rate were better in the posterior than the anterior approach surgery group. The disease
duration and vertebral canal volume were found to be risk factors for ISI in CSM patients.

Conclusion:
Among patients with CSM, the prognosis is worse for those with ISI than those without
ISI. Posterior cervical decompression surgery produces a better curative effect than anterior cervical
decompression surgery in CSM patients with ISI. CSM patients with longer disease duration
and small vertebral canal volume should undergo surgical treatment as early as possible.
Chalcone-thiosemicarbazone Hybrids as Inhibitors of Human Hepatocellular
Carcinoma HepG2 Cells Viability and Oxygen Consumption
Authors: Rodrigues Vivian Cordeiro , Felippe William Queiroz , Goulart Carla Marins , Echevarria Aurea , da Silva Ana Paula Pereira 
Published: January 2022

Background:
Chalcones are open-chain flavonoids especially attractive to medicinal
chemistry due to their easy synthesis and the possibility of structural modifications.

Objective:
This study aims to evaluate the in vitro anticancer activity of a series of hybrids chalcones-
thiosemicarbazones against the human hepatocellular carcinoma cell line HepG2.

Methods:
Seven hybrid chalcones-thiosemicarbazones (CTs), 3-(4’-X-phenyl)-1-phenylprop-
2-en-1-one thiosemicarbazone, where X=H (CT-H), CH3 (CT-CH3), NO2 (CT-NO2), Cl (CTCl),
CN (CT-CN), F (CT-F), and Br (CT-Br), were synthesized and their effects on cells’ viability
and mitochondrial oxygen consumption were assessed.

Results:
Incubation with CTs caused a decrease in HepG2 cells viability in a time-concentration-dependent
manner. The most effective compounds in inhibiting cell viability, after 24 hours of treatment,
were CT-Cl and CT-CH3 (IC50 20.9 and 23.63 μM, respectively). In addition, using 10 μM
and only 1 hour of pre-incubation, CT-CH3 caused a reduction in basal respiration (-37 %), oxygen
consumption coupled with ATP synthesis (-60 %), and maximum oxygen consumption (-54 %). These
alterations in respiratory parameters may be involved with the inhibitory effects of CT-CH3
since significant changes in oxygen consumption rates were observed in a condition that anticipates
more significant losses of cell viability. The ADME parameters and the no violation of Lipinski
Rule of Five showed that all compounds are safe.

Conclusion:
These results may contribute to the knowledge about the effects of CTs on these cells
and the development of new treatments against HCCs.
Bioactive Extracts: Strategies to Generate Diversified Natural Product-
Like Libraries
Authors: Aggarwal Meenu , Singh Raman , Ahlawat Priyanka , Singh Kuldeep 
Published: January 2022

Abstract:
Natural products have stimulated the interest of chemists owing to their abundant structural
diversity and complexity. Indeed, natural products have performed an essential role, particularly
in the cure of cancerous and infectious diseases, thereby providing medicinal researchers with
several unexplored chemotypes for the innovation of new drugs. Fusion of chemical derivatization
and combinatorial synthesis forms the basis of the concept of chemo diversification of plants. Diverse
libraries of natural product analogs are constructed through existing biological and chemical
approaches using unique schemes to expand natural product frameworks. This review aims to present
several approaches employed to offer innovative opportunities to synthesize NP-inspired compound
libraries. Reactive molecular fragments present in most natural products are chemically
converted to chemically engineered extracts (CEEs) or semisynthetic compounds constituting distinct
libraries. Bio-guided isolation for natural products required vital tools like reverse phase
chromatography and bioautographic assays. Different established strategies from DTS, BIOS, CtD,
FOS, FBDD to late-stage diversification facilitate the expansion of molecules with physicochemical
properties. In particular, fragment-like natural products with novel skeletons may be used as
preliminary points for chemical biology and medicinal chemistry programs with great capacity. In
this review, we sum up how NPs have proven fruitful for the novel methodologies responsible for
the diversification of complex natural products; therefore, it is worth going over the upcoming
integration of natural products with combinatorial chemistry.
Investigation of Antiblastic and Antibacterial Properties of Binuclear Platinum
(II)-Interferon Conjugate
Authors: Plotnikov Evgenii , Plotnikov Vladimir 
Published: January 2022

Introduction:
This work aimed to create a new platinum-interferon conjugate and investigate
its properties.

Background:
Multiple drug resistance of tumor cells is a serious challenge in modern medicine.
Neoplastic diseases are often complicated by persistent bacterial infections, which impairs efficacy
and the outcome of anticancer therapy. The development of new bifunctional drugs for the treatment
of tumor growth and bacterial complications is an urgent task.

Objective:
The objective of this study was to evaluate the complex antiblastic and antibacterial
properties of interferon-platinum conjugate in vitro.

Material and Methods:
The coordination complex of dichloro-N,N,N,N-tetrakis-(2-aminoethyl)-
1,6-hexamethylenediaminobisplatin dichloride was used for production of conjugate with
human α-interferon. The binding of a metal complex with protein was established by means of radiochemical
neutron activation analysis. As test objects, we used lympholeukemic Jurkat cells line,
human lymphocytes in reaction of lymphocyte blastic transformation and different strains of microorganisms,
including Staphylococcus aureus and Pseudomonas aeruginosa.

Results:
Binuclear platinum human α-interferon conjugate has a significant dose-dependent
antibacterial and antiproliferative suppressive effect on target cells and bacteria.

Conclusion:
The tested preparation can be of a certain interest in drug designing for rational antiblastic
therapy, especially in the case of infectious complications. This conjugate can be a convenient
platform for creating drugs for the complex therapy of oncological diseases with bacterial
complications.
Neuroprotective Potential of Bacopa monnieri: Modulation of Inflammatory
Signals
Authors: Reale Marcella , Costantini Erica , Jarlapoodi Srinivas , Serra Federica , Aielli Lisa , Khan Haroon , Belwal Tarun , Falasca Katia 
Published: January 2022

Background:
To date, much evidence has shown the increased interest in natural
molecules and traditional herbal medicine as alternative bioactive compounds to fight many inflammatory
conditions, both in relation to immunomodulation and in terms of their wound healing potential.
Bacopa monnieri is a herb that is used in the Ayurvedic medicine tradition for its anti-inflammatory
activity.

Objective:
In this study, we evaluate the anti-inflammatory and regenerative properties of the Bacopa
monnieri extract (BME) in vitro model of neuroinflammation.

Methods:
Neuronal SH-SY5Y cells were stimulated with TNFα and IFNγ and used to evaluate the
effect of BME on cell viability, cytotoxicity, cytokine gene expression, and healing rate.

Results:
Our results showed that BME protects against the Okadaic acid-induced cytotoxicity in
SH-SY5Y cells. Moreover, in TNFα and IFNγ primed cells, BME reduces IL-1β, IL-6, COX-2,
and iNOS, mitigates the mechanical trauma injury-induced damage, and accelerates the healing of
wounds.

Conclusion:
This study indicates that BME might become a promising candidate for the treatment
of neuroinflammation.
Usefulness of 99mTc-Pertechnetate SPECT-CT in Thyroid Tissue Volumetry:
Phantom Studies and a Clinical Case Series
Authors: Calandri Enrico , Giraudo Maria Teresa , Sirovich Roberta , Ostan Antonella , Pultrone Mirco , Frantellizzi Viviana , Conversano Lucia , Bagnasacco Paolo , Gallina Sonya , Vincentis Giuseppe De 
Published: January 2022

Background:
An accurate measurement of the target volume is of primary importance
in theragnostics of hyperthyroidism.

Objective:
Our purpose was to evaluate the accuracy of a threshold-based isocontour extraction procedure
for thyroid tissue volumetry from SPECT-CT.

Methods:
Cylindrical vials with a fixed volume of 99mTcO4 at different activities were inserted into
a neck phantom in two different thickness settings. Images were acquired by orienting the phantom
in different positions, i.e., 40 planar images and 40 SPECT-CT. The fixed values of the isocontouring
threshold for SPECT and SPECT-CT were calculated by means of linear and spline regression
models. Mean, Median, Standard Deviation, Standard Error, Mean Absolute Percentage
Error and Root Mean-Square Error were computed. Any difference between the planar method,
SPECT and SPECT-CT and the effective volume was evaluated by means of ANOVA and posthoc
tests. Moreover, planar and SPECT-CT acquisitions were performed in 8 patients with hyperthyroidism,
considering relevant percentage differences greater than > 20% from the CT gold standard.

Results:
Concerning phantom studies, the planar method shows higher values of each parameter
than the other two methods. SPECT-CT shows lower variability. However, no significant differences
were observed between SPECT and SPECT-CT measurements. In patients, relevant differences
were found in 7 out of 9 lesions with the planar method, in 6 lesions with SPECT, but in only
one with SPECT-CT.

Conclution:
Our study confirms the superiority of SPECT in volume measurement if compared
with the planar method. A more accurate measurement can be obtained from SPECT-CT.
Detection of Enterotoxin Genes in Bacillus species Isolated from Cassava
Processing Environment in Nigeria
Authors: Torimiro Nkem , Daramola Oluwafemi B. , Omole Richard K. , Adesina Ifeyimika Z. 
Published: January 2022

Introduction:
The health challenges associated with cassava products as a common staple
food for approximately 70 % of Africans and part of Asia pose a looming danger due to Bacillus
enterotoxins’ presence in the processing environment.

Objective:
This study investigated the presence of enterotoxigenic genes, namely, Bacillus cereus
enterotoxin T (bceT), hemolysin bl (hblC, hblD), and non-haemolytic enterotoxin (nheA, nheB, and
nheC) from Bacillus species isolated from soil of cassava processing environment.

Methods:
Soil samples from 20 cassava processing sites in Ile-Ife and Modakeke, Nigeria, were
collected and cultured on nutrient agar at 37ºC for 24 hours. Colonies phenotypically identified as
Bacillus were identified using Bacillus-specific 16S rRNA-targeted PCR technique. Screened Bacillus
spp were assessed for the presence of enterotoxigenic genes using PCR with previously reported
primers.

Results:
A total of 100 Bacillus isolates were selected from this study, with Bacillus macerans (33
%) showing the highest frequency of occurrence among the identified species, however, 74 isolates
were molecularly confirmed as Bacillus. Amongst the 74 molecularly confirmed Bacillus isolates,
28 (37.84 %), 35 (47.30 %), and 37 (50 %) had nhe, hbl, and bceT genes, respectively. Investigation
showed that 42 (56.76 %) of the Bacillus species encoded at least one of the screened enterotoxin
genes.

Conclusion:
The presence of these 3 sets of enterotoxin genes in Bacillus isolated from cassava
processing sites calls for immediate attention as they could be pivotal in the release of toxins in cassava
products, causing lethal effects via consumption. This study demonstrates the possibility of
foodborne disease outbreaks in Bacillus toxin-laden cassava products processed under unhygienic
conditions.
Credit and Recognition for Contributions to Data-Sharing Platforms Among Cohort Holders and Platform Developers in Europe: Interview Study
Authors: Devriendt Thijs , Borry Pascal , Shabani Mahsa 
Published: January 2022

Background
The European Commission is funding projects that aim to establish data-sharing platforms. These platforms are envisioned to enhance and facilitate the international sharing of cohort data. Nevertheless, broad data sharing may be restricted by the lack of adequate recognition for those who share data.

Objective
The aim of this study is to describe in depth the concerns about acquiring credit for data sharing within epidemiological research.

Methods
A total of 17 participants linked to European Union–funded data-sharing platforms were recruited for a semistructured interview. Transcripts were analyzed using inductive content analysis.

Results
Interviewees argued that data sharing within international projects could challenge authorship guidelines in multiple ways. Some respondents considered that the acquisition of credit for articles with extensive author lists could be problematic in some instances, such as for junior researchers. In addition, universities may be critical of researchers who share data more often than leading research. Some considered that the evaluation system undervalues data generators and specialists. Respondents generally looked favorably upon alternatives to the current evaluation system to potentially ameliorate these issues.

Conclusions
The evaluation system might impede data sharing because it mainly focuses on first and last authorship and undervalues the contributor’s work. Further movement of crediting models toward contributorship could potentially address this issue. Appropriate crediting mechanisms that are better aligned with the way science ought to be conducted in the future need to be developed.
Transformaciones en la identidad femenina, cambio generacional y revolución: primera mitad del siglo XX
Authors: Vasquez Montaño Rosario Margarita 
Published: January 2022

Este artículo identifica y analiza los cambios generacionales que experimentaron las mujeres en su relación con el espacio público y privado en el contexto del posicionamiento del feminismo como un movimiento político e ideológico durante las primeras décadas del siglo XX. A través de la trayectoria de la escritora socialista estadounidense Ethel Duffy Turner, identificamos diferentes ámbitos de transformación que podemos enmarcar dentro del movimiento de emancipación femenina. Mediante el análisis de hemerografía, memorias y a partir de una contextualización histórica e historiográfica, se proponen elementos que permitan identificar el perfil y conformación de las mujeres modernas y sus características.
Comparison of Different Multispectral Images to Map Hydrothermal Alteration Zones in Kokap, Kulon Progo
Authors: Raharja Bayu , Setianto Agung , Titisari Anastasia Dewi 
Published: January 2022

Using remote sensing data for hydrothermal alteration mapping beside saving time and reducing cost leads to increased accuracy. In this study, the result of multispectral remote sensing tehcniques has been compare for manifesting hydrothermal alteration in Kokap, Kulon Progo. Three multispectral images, including ASTER, Landsat 8, and Sentinel-2, were compared in order to find the highest overall accuracy using principle component analysis (PCA) and directed component analysis (DPC). Several subsets band combinations were used as PCA and DPC input to targeting the key mineral of alteration. Multispectral classification with the maximum likelihood algorithm was performed to map the alteration types based on training and testing data and followed by accuracy evaluation. Two alteration zones were succeeded to be mapped: argillic zone and propylitic zone. Results of these image classification techniques were compared with known alteration zones from previous study. DPC combination of band ratio images of 5:2 and 6:7 of Landsat 8 imagery yielded a classification accuracy of 56.4%, which was 5.05% and 10.13% higher than those of the ASTER and Sentinel-2 imagery. The used of DEM together with multispectral images was increase the accuracy of hydrothermal alteration mapping in the study area.