Design, Synthesis, and Biological Evaluation of Triazolopyrimidine-Isatin Hybrids as Promising Candidates for Triple-Negative Breast Cancer.

Triple-negative breast cancer (TNBC) is a highly aggressive subtype marked by pronounced intra-tumoral heterogeneity and frequent therapeutic resistance. In this study, we report the design, synthesis, and biological evaluation of a novel series of triazolopyrimidine-isatin hybrids against the TNBC cell lines MDA-MB-231 and MDA-MB-468. Among them, 9h emerged as the most promising candidate, exhibiting potent cytotoxic activity against TNBC cell lines.

Design, synthesis, and anti-plasmodial profiling of oxalamide-linked 4-aminoquinoline-phthalimide hybrids.

A series of hydrazinyl-oxoacetamide linked 4-aminoquinoline-phthalimides were synthesized and assayed for their anti-plasmodial activities against the chloroquine-resistant W2 strain of . The synthesized compounds exhibited activity in the low nanomolar range with eight compounds being more active than the standard drug, chloroquine (CQ). Structure-activity relationship studies indicated the dependence of anti-plasmodial activity on the length of the alkyl chain used as a spacer with two of the most promising compounds of the series exhibiting an IC value of 0.

Design, Synthesis, and Antiproliferative and Apoptotic Assessment of Triazole-Tethered Bisnaphthalimide-Isatin Hybrids on Triple-Negative Breast and Prostate Cancers.

This study reports the design, synthesis, and biological evaluation of 1H-1,2,3-triazole-tethered bisnaphthalimide-isatin hybrids as potential antiproliferative agents. The compounds are efficiently synthesized via copper-promoted azide-alkyne cycloaddition and assayed against triple-negative breast (MDA-MB-231) and prostate (DU-145) cancer cell lines. Structure-activity relationship studies reveal that halogen substitution and spacer length substantially influenced anticancer activity.

Annular pancreas in adulthood: Two compelling cases, including one with pyloric stenosis and chronic pancreatitis.

We report the infrequent occurrence of the annular pancreas (AP) in adults by presenting two remarkable cases. The first case involved an incidental discovery of an AP in a patient diagnosed with chronic pancreatitis. Surgical intervention was warranted due to gastric outlet obstruction resulting from pyloric stenosis.

Design and Synthesis of Nitroimidazole-Quinoline Derivatives as Potential Therapeutics Specifically against Sexually-Transmitted Anaerobic Protozoal Pathogens.

Protozoal pathogens Trichomonas vaginalis and Tritrichomonas foetus are the causative agents of sexually transmitted diseases like trichomoniasis among humans and cattle, respectively. Metronidazole (a nitroimidazole-based entity) has been used as the preferred drug to treat protozoal infections for the past few years. However, the emergence of resistance has prompted researchers to further explore the nitroimidazole core to overcome its limitations while improving efficacy.

Iron oxide nanoparticles: a versatile nanoplatform for the treatment and diagnosis of ovarian cancer.

Ovarian cancer remains one of the main causes of human mortality, accounting for millions of deaths every year. Despite of several clinical options such as chemotherapy, photodynamic therapy (PDT), hormonal treatment, radiation therapy, and surgery to manage this disease, the mortality rate is still very high. This alarming statistic highlights the urgent need for innovative approaches to improve both diagnosis and treatment.

Design, Synthesis, Anti-Proliferative, and Apoptotic Assessment of Spirocyclopropyl Oxindole-Isatin Hybrids on Triple-Negative Breast Cancer.

A series of 1H-1,2,3-triazole-tethered spirocyclopropyl oxindole-isatin hybrids were synthesized using a copper-promoted click reaction and evaluated for their anti-proliferative activities against triple-negative breast cancer cell lines. The most potent compound in the series outperformed tamoxifen and 5-fluorouracil, with selectivity indices of 1.60 and 1.

Design analysis and performance enhancement of a 2-element MIMO skin-implantable antenna for IoT-based health monitoring devices.

Two two-element slotted patch multiple-input multiple-output (MIMO) antenna with coplanar waveguide (CPW) feed is proposed for deployment in implantable medical devices. Implantable devices are compact and demand high-gain antennae with unidirectional radiation patterns. Regarding compactness, the antenna has a size of 16 × 6×0.

Design, Synthesis, and Anti-Mycobacterial Evaluation of Triclosan-Isoniazid Hybrids.

A series of Triclosan-based hybrids and their Schiff base derivatives with isoniazid were designed through in silico modeling and synthesized using copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. These compounds were then evaluated against both Mycobacterium tuberculosis (Mtb) and Mycobacterium abscessus (Mab). However, none of the synthesized hybrids exhibited significant growth inhibition, with minimum inhibitory concentration (MIC) values consistently exceeding 100 µg/mL.

Design, synthesis and mechanistic exploration of anti-plasmodial Indolo[2,3-]quinoxaline-7-chloroquinoline hybrids.

The aim of this study is to synthesize indolo[2,3-]quinoxaline-4-aminoquinoline-based hybrids and evaluate their effectiveness against chloroquine-susceptible (3D7) and resistant (W2) strains, with expected inhibition of chloroquine resistance transporter (CRT) and heme. The hybrids were synthesized and evaluated against both susceptible and resistant strains. Molecular docking and studies were conducted to assess the binding affinities for the CRT protein.

Design, synthesis and mechanistic insights into triclosan derived dimers as potential anti-plasmodials.

In pursuit of novel anti-plasmodial agents, a library of triclosan-based dimers both with and without a 1-1,2,3 triazole core were designed and synthesized in order to achieve a multitargeted approach. assessment against chloroquine-susceptible (3D7) and resistant (W2) strains identified that two of the synthesized dimers containing triazole were the most potent in the series. The most potent of the synthesized compounds exhibited IC values of 9.

Cu-promoted synthesis of triclosan-Mannich and Glaser adducts: anti-mycobacterial evaluation with validations.

 The WHO, Global tuberculosis report 2022 estimated number of tuberculosis (TB) cases reached 10.6 million in 2021, reflecting a 4.5% increase compared with the 10.

Strategic Analysis of Collaborative Networks in Spodoptera frugiperda (Lepidoptera: Noctuidae) Research for Improved Pest Management Strategies.

The fall armyworm (FAW) poses a significant global threat to food security, and economics. Timely detection is crucial, and this research explores innovative techniques like data analysis, remote sensing, satellite imagery, and AI with machine learning algorithms for predicting and managing outbreaks. Emphasizing the importance of community engagement and international collaboration, social network analysis (SNA) is employed to uncover collaborative networks in FAW management research.

Association between Covishield vaccine and menstrual disturbance. Findings from a cross-sectional study among participants of Zero TB cohort in India.

Background: The association between covid-19 vaccine and menstrual disturbance is unclear.

Methods: An in-person cross-sectional survey among female members ≥ 18 years enrolled in an ongoing Zero TB prospective cohort in Northern India who had received one or two doses of covid-19 vaccine was conducted to study the characteristics and association of menstrual disturbance within six months of receiving Covishield.

Results: Between June 29 and September 5, 2021, 339 females ≥ 18 years of age were administered the survey.

Rational Design and Synthesis of Isatin-Chalcone Hybrids Integrated with 1H-1,2,3-Triazole: Anti-Proliferative Profiling and Molecular Docking Insights.

In this study, a series of isatin-chalcone linked triazoles were synthesized using Cu-promoted Azide-Alkyne Cycloaddition (CuAAC) reaction and evaluated for their cytotoxicity against various cancer cell lines. The most potent compound displayed approximately 2.5 times greater activity compared to both reference compounds against ovarian cancer cell lines.

Sustainable Harnessing of Waste Polycarbonate for Synthesizing Activated Furans to Generate Stenhouse Adducts on Polymer Surface.

Plastics are versatile materials, offering lightweight, durable, and affordable solutions across various industries. However, their non-degradable nature poses challenges by end of their life. This study presented an innovative carbonyl extraction method to utilize waste poly(bisphenol A carbonate) (PC) as reaction precursor to synthesis of activated furan as precursor for photoswitchable Stenhouse adducts.

Amphiphilic, lauric acid-coupled pluronic-based nano-micellar system for efficient glipizide delivery.

Glipizide; an insulin secretagogue belonging to the sulfonylurea class, is a widely used antidiabetic drug for managing type 2 diabetes. However, the need for life-long administration and repeated doses poses challenges in maintaining optimal blood glucose levels. In this regard, orally active sustained-release nano-formulations can be a better alternative to traditional antidiabetic formulations.

Percutaneous Tenotomy for Chronic Tennis Elbow: A Minimally Invasive Technique with Better Outcomes - A Case Series.

Background: Tennis elbow (lateral epicondylitis elbow) is a self-limiting disease of indeterminate pathogenesis. Conservative therapy is the treatment of choice. In chronic tennis elbow with failure of conservative therapy; surgical treatment is a method of choice.

Design and performance analysis of an L-shaped radiator and defected ground antenna for enhancing wireless connectivity in brain implants.

Brain implantable wireless microsystems has potential to treat neurological diseases and maintain the quality of life. Highly efficient miniaturized antenna is the fundamental part of BID (brain implantable device) for reliable signaling of data through dissipative intracranial material. In this paper, a patch antenna with L-shaped defected ground is demonstrated.

Tailoring selective triclosan azo-adducts: Design, synthesis, and anti-mycobacterial evaluation.

A series of triclosan azo-adducts were synthesized to investigate their structure-activity relationship against and non-tuberculous mycobacteria. The series' most potent compound was four and sixteen times more active than triclosan and rifabutin against drug-resistant , respectively, while being less cytotoxic to human macrophages than triclosan on day one. Additionally, one of the azo-adducts was twice as efficient against as triclosan and twice as effective against as isoniazid.

Isatin-indoloquinoxaline click adducts with a potential to overcome platinum-based drug-resistance in ovarian cancer.

Herein, a series of isatin tethered indolo[2,3-b]quinoxaline hybrids was synthesized by considering the pharmacophoric features of known DNA intercalators and topoisomerase II inhibitors. The anti-proliferative properties of the synthesized compounds were evaluated against ovarian cancer cell lines (SKOV-3 and Hey A8). Four of the compounds exhibited promising anti-proliferative activities, with one of them being 10-fold more potent than cisplatin against drug-resistant Hey A8 cells.

Special Issue "Hybrid Drugs: Design and Applications".

The widely held belief in the potential superiority of agents capable of modulating multiple biological targets has led to the adoption of molecular hybridization as an effective technique in the realm of drug discovery and development [...

Stereo/regio-selective access to substituted 3-hydroxy-oxindoles with anti-proliferative assessment and validation.

The manuscript focuses on a highly stereo-/regioselective approach for synthesizing a diverse array of substituted-3-hydroxy-2-oxindoles. The synthesized compounds were subsequently subjected to anti-proliferative assessment against various cell lines, including colorectal carcinoma, ovarian cancer, and human metastatic melanoma cancer. The structural characterization of the synthesized scaffolds was unambiguously confirmed using X-ray diffraction analysis.