A novel sulfamoylphenyl-dihydro-thiadiazole derivative as a dual EGFR and carbonic anhydrase inhibitor for cancer therapy.

A novel sulfamoylphenyl-dihydro-thiadiazole derivative (compound 14) has been designed and synthesized as a dual inhibitor targeting EGFR and human carbonic anhydrases (hCA_IX and hCA_XII). Computational studies, including density functional theory (DFT), molecular docking, and molecular dynamics simulations, confirmed its stability, favorable binding interactions, and reactivity profiles. Compound 14 showed potent inhibition of EGFR (IC₅₀ = 10.

Discovery of new thiadiazole-based VEGFR-2 inhibitors: design, synthesis, cytotoxicity, and apoptosis induction.

Background: Vascular endothelial growth factor receptor-2 (VEGFR-2) is a validated target in cancer therapy. However, approved inhibitors like sorafenib are often limited by off-target toxicity and resistance. This study aimed to develop novel thiadiazole-based VEGFR-2 inhibitors with improved selectivity and safer profiles.

Integrated computational and biological evaluations of newly synthesized thiadiazole-based VEGFR-2 inhibitors with targeted anti-breast cancer activity.

The development of novel VEGFR-2 inhibitors remains a promising strategy for targeted breast cancer therapy, particularly against aggressive triple-negative breast cancer subtype. In this study, a series of thiadiazole derivatives were designed, synthesized, and biologically evaluated for their anti-proliferative activity against MDA-MB-231 and MCF-7 breast cancer cell lines. Among them, compound 7 exhibited superior cytotoxicity (IC₅₀ = 5.

New Thiadiazole-Benzenesulfonamide Hybrids as Dual B-Raf/VEGFR-2 Inhibitors With Promising Anti-Hepatic Cancer Activity.

A new group of thiadiazole-benzenesulfonamide hybrids was designed, synthesized, and biologically evaluated as potential dual inhibitors targeting B-Raf and VEGFR-2 for cancer therapy. The cytotoxic activity of the synthesized derivatives was assessed against HepG2 and Huh7 liver cancer cell lines, where compound 7a exhibited the most potent activity with IC values of 17.89 μM and 25.

Development of New Thiadiazole Derivatives as VEGFR-2 Inhibitors With Anticancer and Proapoptotic Activities‏.

A series of thiadiazole-based derivatives were synthesized and evaluated for their potential as VEGFR-2 inhibitors and anticancer agents. Among them, compound 7b demonstrated significant cytotoxic activity against MCF-7 breast cancer cells, with an IC value of 6.13 µM, surpassing that of the reference drug sorafenib (IC: 7.

Novel furo[2,3-]pyrimidine derivatives as PI3K/AKT dual inhibitors: design, synthesis, biological evaluation, and molecular dynamics simulation.

The current study aimed to synthesize a series of innovative improved anticancer chemical entities by combining the unique advantages of 1,3,4-thiadiazole as an established anticancer pharmacophore with the furopyrimidine scaffold which is a key component of many reported cytotoxic agents. Sixteen furopyrimidine derivatives were designed and evaluated by several biological tests including antiproliferative activity against 60 human cancer cell lines, measurement of GI, TGI, and LC values, MTT and selectivity index (SI) calculation, enzymatic PI3Kα/β and AKT inhibitory assay, cell cycle analysis and apoptosis evaluation. The results indicated that the designed compound 10b revealed potent anticancer activity with a mean GI of 108.

Development of new anticancer thiadiazole-sulfonamides as dual EGFR/carbonic anhydrase inhibitors.

Background: Thiadiazole-sulfonamide derivatives were synthesized as dual inhibitors of epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX) to develop selective anticancer agents.

Methods: Cytotoxicity was evaluated against MDA-MB-231 and MCF-7 breast cancer cells, with selectivity tested on Vero cells. Enzymatic inhibition studies were conducted against EGFR and CA-IX, using erlotinib and acetazolamide as reference drugs.

New nicotinamide-thiadiazol hybrids as VEGFR-2 inhibitors for breast cancer therapy: design, synthesis and and evaluation.

Vascular endothelial growth factor receptor-2 (VEGFR-2) is a key regulator of tumor angiogenesis and has become an important target in anticancer drug development. In this study, novel nicotinamide-thiadiazol hybrids were synthesized and evaluated for their anti-breast cancer potential through VEGFR-2 inhibition. The compounds were assessed for their cytotoxicity against MDA-MB-231 and MCF-7 cell lines.

Thiadiazole chitosan conjugates as a novel cosmetic ingredient for rinse-off hair conditioners: design, formulation, characterization and in silico-molecular docking studies.

Recently, chitosan derivatives, as eco-sustainable and renewable products, have been recorded to be highly effective toward cosmetics with potent biological activity. The main core of this research is to develop an organic hair conditioner (OHC) based on two chitosan-thiadiazole conjugates, chitosan-(ethylthio‑thiadiazole) (CH-ETD) and chitosan-(benzylthio‑thiadiazole) (CH-BTD), with natural fragrances. A series of nine OHC formulae were prepared (CH1-CH3 for chitosan based OHC, E1-E3 for CH-ETD based OHC, and B1-B3 for CH-BTD based OHC) and characterized based on their visual examination, pH, thermal stability, dirt dispersion, moisturizing time, percentage of solid content, hair irritation, rinsing, combing, and the luster.

Design and synthesis of thiadiazoles as anticancer, apoptotic, and VEGFR-2 inhibitors.

Background: Vascular endothelial growth factor receptor (VEGFR-2) inhibitors are critical in cancer therapy due to their role in suppressing tumor angiogenesis. Herein, we report a new series of thiadiazole-based derivatives as potential VEGFR-2 inhibitors with promising anticancer activity.

Methods: The synthesized compounds were evaluated for anti-proliferative activity against human cancer cell lines (HCT-116, MCF-7, and HepG-2), and WI-38 as normal cells.

Unraveling the interaction of pyranocoumarins with P-glycoprotein: Implications for overcoming multidrug resistance in cancer therapy.

This study aimed to investigate the antiproliferative activity and P-glycoprotein (P-gp) inhibitory potential of a series of novel pyranocoumarin derivatives. Compounds 4a-c and 4f-i showed the most potent activity against MCF-7 (breast cancer), MCF-7/ADR (human breast cancer cell) resistant to Adriamycin (ADR), and Caco-2 (colon carcinoma) cell lines compared to Sorafenib and Doxorubicin, while all the compounds 4a-i demonstrated week growth inhibitory impact toward two normal cell lines, HFL-1 and WI-38 with IC values between 56.5 and 81.

Structure-Performance Relationship of Novel Azo-Salicylaldehyde Disperse Dyes: Dyeing Optimization and Theoretical Insights.

High yields of three novel azo disperse dyes based on the diazonium salt of sulfonamides-azo-salicylaldehyde were successfully synthesized. These dyes were structurally characterized by using spectroscopic techniques, including FTIR, H NMR, and MS. The fundamental goal of the research was to determine the optimal dyeing parameters, such as temperature, pH, and time, to understand the behavior of dispersed dyes - during the dyeing of polyester materials.

Novel Azo dyes containing a hydrazide-hydrazone moiety for dyeing polyester fabric.

Novel azo dyes containing a hydrazide-hydrazone moiety linked to the benzothiazole nucleus are synthesized effectively in this study. The primary purpose of the study was to identify the best dyeing parameters, such as shade, temperature, pH, and time, in order to better understand the behaviour of dispersed dyes during polyester dyeing. To achieve excellent colour strength in value (K/S = 26), the ideal dyeing conditions for disperse dye 4 were 30 min, pH of 8, and 110 °C at shade 3%.

Design, synthesis, and evaluation of novel thiadiazole derivatives as potent VEGFR-2 inhibitors: a comprehensive and study.

Objective: This study aims to investigate the potential of designed 2,3-dihydro-1,3,4-thiadiazole derivatives as anti-proliferative agents targeting VEGFR-2, utilizing a multidimensional approach combining and analyses.

Methods: The synthesized derivatives were evaluated for their inhibitory effects on MCF-7 and HepG2 cancer cell lines. Additionally, VEGFR-2 inhibition was assessed.

Anti-proliferative 2,3-dihydro-1,3,4-thiadiazoles targeting VEGFR-2: Design, synthesis, in vitro, and in silico studies.

In this study, we present the design, synthesis, and evaluation of six new thiadiazole derivatives designed as VEGFR-2 inhibitors. The most promising compound, 18b, demonstrated promising inhibitory activity against VEGFR-2, with an IC value of 0.165 µg/mL.

Thiazolation of phenylthiosemicarbazone to access new thiazoles: anticancer activity and molecular docking.

Novel thiazole hybrids were synthesized via thiazolation of 4-phenylthiosemicarbazone (). The anticancer activity against the NCI 60 cancer cell line panel. Methyl 2-(2-((1-(naphthalen-2-yl)ethylidene)hydrazineylidene)-4-oxo-3-phenylthiazolidin-5-ylidene)acetate () showed significant anticancer activity at 10 μM with a mean growth inhibition (GI) of 51.

Fabrication and characterization of a new eco-friendly sulfonamide-chitosan derivative with enhanced antimicrobial and selective cytotoxicity properties.

Chitosan (CH) exhibits low antimicrobial activity. This study addresses this issue by modifying the chitosan with a sulfonamide derivative, 3-(4-(N,N-dimethylsulfonyl)phenyl)acrylic acid. The structure of the sulfonamide-chitosan derivative (DMS-CH) was confirmed using Fourier transform infrared spectroscopy and Nuclear magnetic resonance.

Design, synthesis, and anticancer evaluation of N-sulfonylpiperidines as potential VEGFR-2 inhibitors, apoptotic inducers.

A new panel of N-sulfonylpiperidine derivatives has been designed and synthesized as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. Anti-proliferative activities of the synthesized members were tested against colorectal carcinoma (HCT-116), hepatocellular carcinoma (HepG-2), and breast cancer (MCF-7) cell lines. Compounds 3a, 4, 8, and 9 showed the highest activities against the tested cell lines.

Novel Monosulfonated Azo Dyes: Design, Synthesis, and Application as Disperse Dyes on Polyester Fabrics.

This study synthesizes and characterizes a series of disperse dyes based on azo Schiff bases, compounds -. Their structures were identified using various analytical techniques, such as FT-IR, H/C NMR, and mass spectrometry. The study's primary objective was to investigate the behavior of disperse dyes - when used for dyeing polyester fabrics under different conditions, including variations in time, temperature, shade, and pH.

Rationale design and synthesis of new apoptotic thiadiazole derivatives targeting VEGFR-2: computational and studies.

This work presents the synthesis and , and analyses of new thiadiazole derivatives that are designed to mimic the pharmacophoric characteristics of vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. A comprehensive evaluation of the inhibitory properties of the synthesized thiadiazole derivatives against the cancer cell lines MCF-7 and HepG2 identified several auspicious candidates. Among them, compound 14 showed remarkably low IC values of 0.

Introducing of novel class of pyrano[2,3-]pyrazole-5-carbonitrile analogs with potent antimicrobial activity, DNA gyrase inhibition, and prominent pharmacokinetic and CNS toxicity profiles supported by molecular dynamic simulation.

Microbiological DNA gyrase is recognized as an exceptional microbial target for the innovative development of low-resistant and more effective antimicrobial drugs. Hence, we introduced a one-pot facile synthesis of a novel pyranopyrazole scaffold bearing different functionalities; substituted aryl ring, nitrile, and hydroxyl groups. All new analogs were characterized with full spectroscopic data.

Synthesis, description, and application of novel corrosion inhibitors for CS AISI1095 in 1.0 M HCl based on benzoquinoline derivatives.

This study aims to synthesize and evaluate the corrosion inhibition properties of three newly prepared organic compounds based on benzo[h]quinoline hydrazone derivatives. The compounds structure were characterised using FTIR, 1H-NMR, 13C-NMR and Mass spectroscopy. Electrochemical methods, including Potentiodynamic Polarization (PP), Electrochemical Frequency Modulation (EFM), and Electrochemical Impedance Spectroscopy (EIS) were employed to evaluate the compounds as corrosion inhibitors in HCl (1.

Synthesis, characterization, and biological evaluation of new chitosan derivative bearing diphenyl pyrazole moiety.

This work reports the synthesis of a new pyrazole derivative by reacting 5-amino-1,3-diphenyl pyrazole with succinic anhydride and bearing the product chemically on the chitosan chains via amide linkage to achieve a new chitosan derivative (DPPS-CH). The prepared chitosan derivative was analyzed by IR, NMR, elemental analysis, XRD, TGA-DTG, and SEM. As compared with chitosan, DPPS-CH showed an amorphous and porous structure.

New thiadiazole modified chitosan derivative to control the growth of human pathogenic microbes and cancer cell lines.

The emergence of multidrug-resistant microbes and the propagation of cancer cells are global health issues. The unique properties of chitosan and its derivatives make it an important candidate for therapeutic applications. Herein, a new thiadiazole derivative, 4-((5-(butylthio)-1,3,4-thiadiazol-2-yl) amino)-4-oxo butanoic acid (BuTD-COOH) was synthesized and used to modify the chitosan through amide linkages, forming a new thiadiazole chitosan derivative (BuTD-CH).