Indoles as promising Therapeutics: A review of recent drug discovery efforts.

Indole, a fundamental heterocyclic core, has emerged as a cornerstone in the medicinal chemistry due to its diverse biological activities and structural versatility. This aromatic compound, present in natural as well as synthetic compounds, offers a versatile platform for the drug discovery. By strategically incorporating functional groups or pharmacophores, researchers can tailor indole-derivatives to target a wide range of diseases.

PROTAC unleashed: Unveiling the synthetic approaches and potential therapeutic applications.

Proteolysis-Targeting Chimeras (PROTACs) are a novel class of bifunctional small molecules that alter protein levels by targeted degradation. This innovative approach uses the ubiquitin-proteasome system to selectively eradicate disease-associated proteins, providing a novel therapeutic strategy for a wide spectrum of diseases. This review delineates detailed synthetic approaches involved in PROTAC building blocks, including the ligand and protein binding parts, linker attached structural components of PROTACs and the actual PROTAC molecules.

Effects of Linkers and Substitutions on Multitarget Directed Ligands for Alzheimer's Diseases: Emerging Paradigms and Strategies.

Alzheimer's disease (AD) is multifactorial, progressive and the most predominant cause of cognitive impairment and dementia worldwide. The current "one-drug, one-target" approach provides only symptomatic relief to the condition but is unable to cure the disease completely. The conventional single-target therapeutic approach might not always induce the desired effect due to the multifactorial nature of AD.

Benzimidazole-based fluorophores for the detection of amyloid fibrils with higher sensitivity than Thioflavin-T.

Protein aggregation into amyloid fibrils is a key feature of a multitude of neurodegenerative diseases such as Alzheimer's, Parkinson's, and Prion disease. To detect amyloid fibrils, fluorophores with high sensitivity and better efficiency coupled with the low toxicity are in high demand even to date. In this pursuit, we have unveiled two benzimidazole-based fluorescence sensors ([C H N ] (C1) and [C H N O ] (C2), which possess exceptional affinity toward different amyloid fibrils in its submicromolar concentration (8 × 10  M), whereas under a similar concentration, the gold standard Thioflavin-T (ThT) fails to bind with amyloid fibrils.

Mitigation of NOx and smoke emissions in a diesel engine using novel emulsified lemon peel oil biofuel.

Lemon peel oil (LPO) is considered to be a viable alternative fuel for diesel engine applications due to its wider availability, renewable nature, easy extraction process, almost equivalent calorific value as neat diesel, and low viscosity. The present work aims to investigate the effect of novel emulsified LPO in a diesel engine in order to reduce the NOx emission without compromising the engine performance. A new ionic surfactant is introduced in the present study, namely methyl-dihydroxy propyl imidazolium chloride due to its higher hydrophilic-lipophilic balance value which helps to prepare stable water in oil emulsion.

Is [F-18]-fluorodeoxyglucose FDG-PET/CT better than ct alone for the preoperative lymph node staging of muscle invasive bladder cancer?

Objective: To evaluate whether the use of [F-18]-FDG-PET/CT can accurately predict pelvic lymph node metastasis in patients with muscle invasive TCC of the bladder undergoing radical cystectomy.

Materials And Methods: Fifteen patients with muscle invasive bladder cancer had undergone FDG-PET/CT scan from the skull base to the mid-thighs after IV injection of 6.5MBq (Mega-Becquerel)/Kg of FDG.

Scrutinizing the DNA damaging and antimicrobial abilities of triazole appended metal complexes.

New mononuclear transition metal complexes 1-12 bearing the bioactive triazole analogues were synthesized and characterized by elemental analysis and spectroscopic techniques. The interaction of calf thymus DNA (CT-DNA) with the synthesized compounds was studied at physiological pH by spectrophotometric, spectrofluorometric, cyclic voltammetry, and viscometric techniques. The entire DNA binding results suggested the intercalative mode of binding for the synthesized compounds.

Exploring the photochemosensitivity by novel cysteine-based mixed ligand complexes.

A new series of cysteine-based metal(II) complexes with 2,2'-bipyridine or 1,10-phenanthroline as co-ligand have been prepared and characterized. Their DNA binding and cleavage properties have been studied. The analytical and spectroscopic data of complexes 1-18 reveal that the complexes adopt an octahedral geometry around the central metal ion in which the cysteine is coordinated through NS and NN atoms, respectively.

Persistent DNA binding, cleavage performance and eco-friendly catalytic nature of novel complexes having 2-aminobenzophenone precursor.

This paper describes the synthesis of four novel bidentate metal(II) complexes having 2-aminobenzophenone precursor and a co-ligand (anthranilic acid). They are characterized by the usual spectral and analytical data. They adopt octahedral geometrical arrangements around the metal ions which have been confirmed by electronic absorption data.

Targeting protein kinase and DNA molecules by diimine-phthalate complexes in antiproliferative activity.

The serendipitous discovery of the anticancer drug cisplatin cemented medicinal inorganic chemistry as an independent discipline in 1960s. DNA and protein kinases are one of the major intracellular targets of many anticancer drugs. It is thus highly desirable to develop metal complexes, either by interacting with DNA or to target alternative cellular machinery such as protein kinases to provide a more effective means of monitoring disease progression.

Investigation of in vitro anticancer and DNA strap interactions in live cells using carboplatin type Cu(II) and Zn(II) metalloinsertors.

A series of carboplatin type Cu(II) and Zn(II) metalloinsertors (1-8) having β-diketone analogues and biologically significant cyclobutane-1,1-dicarboxylic acid have been synthesized and characterized by spectral and analytical methods. The binding and cleavage propensity of these metalloinsertors on DNA and their cytotoxic effects in live cells have been explored. From the gel electrophoresis study, it is observed that the complexes 1-8 cleave pBR322 DNA via a hydrolytic mechanism induced by hydroxyl radical scavengers, DMSO and EtOH as the reactive oxygen species (ROS).

Photo biological activation of NSO donor mixed-ligand complexes: in vivo and preclinical perspectives.

Pyrazolone incorporating N-acetylcysteine (NAC) mixed-ligand complexes are described as promising anti-inflammatory, anticonvulsant, SODs mimetic and cytotoxic compounds possibly due to its antioxidant profile. In this study, we have evaluated the pharmacologic activity, antioxidant and toxicological profiles of compounds (1-6). Among them, compounds 1 and 4 were haemobiocompatible than the others.

DNA fastening and ripping actions of novel Knoevenagel condensed dicarboxylic acid complexes in antitumor journey.

Few novel Cu(II) and Zn(II) oxali-platin type complexes of stoichiometry [ML(ox)] where, L is a Knoevenagel ligand and ox is oxalic acid, have been explored. They are well characterized by spectroanalytical methods. The binding and cleavage propensity of these complexes on DNA and their cytotoxic effect in tumor cells have been investigated.

Exploring DNA binding and nucleolytic activity of few 4-aminoantipyrine based amino acid Schiff base complexes: a comparative approach.

A series of novel Co(II), Cu(II), Ni(II) and Zn(II) complexes were synthesized from Schiff base(s), obtained by the condensation of 4-aminoantipyrine with furfural and amino acid (glycine(L1)/alanine(L2)/valine(L3)) and respective metal(II) chloride. Their structural features and other properties were explored from the analytical and spectral methods. The binding behaviors of the complexes to calf thymus DNA were investigated by absorption spectra, viscosity measurements and cyclic voltammetry.

Lasing the DNA fragments through β-diketimine framed Knoevenagel condensed Cu(II) and Zn(II) complexes--an in vitro and in vivo approach.

The syntheses, structures and spectroscopic properties of Cu(II) and Zn(II) complexes having Knoevenagel condensate β-diketimine Schiff base ligands have been investigated in this paper. Characterization of these complexes was carried out using FTIR, NMR, UV-Vis, elemental analysis, mass and EPR techniques. Absorption titration, electrochemical analyses and viscosity measurements have also been carried out to determine the mode of binding.

Pithecellobium dulce mediated extra-cellular green synthesis of larvicidal silver nanoparticles.

Present study reports a green chemistry approach for the biological synthesis of silver nanoparticles using the aqueous leaf extract of Pithecellobium dulce, which acts as a reducing and capping agent. It is observed that use of P. dulce leaf extract makes a fast, environmentally benign and convenient method for the synthesis of silver nanoparticles and can reduce silver ions into silver nanoparticles.

Villous adenoma of the ampulla of Vater.

A case of villous adenoma of the ampulla of Vater in a 40 year old male is described. The clinical significance of this rare tumour is discussed and the relevant literature reviewed.