Pyrrolidine derivatives as α-amylase and α-glucosidase inhibitors: Design, synthesis, structure-activity relationship (SAR), docking studies and HSA binding.

In our pursuit of developing effective inhibitors for the enzymes α-amylase and α-glucosidase, which play a crucial role in carbohydrate metabolism related to type-2 diabetes, we synthesized compounds featuring a pyrrolidine ring. The synthesis involved coupling N-Boc-proline with various aromatic amines, resulting in the formation of distinct N-Boc proline amides. To investigate the influence of the Boc group on enzyme inhibition, the Boc group was subsequently removed.

Future Roadmaps for the Treatment of Guinea Worm Disease: Progress in Synthetic and Green Approaches.

For decades, guinea worm disease, caused by the parasitic worm Dracunculus medinensis, has been a major public health concern, impacting vulnerable populations in Africa and Asia. This review gives an in-depth examination of the various therapeutic approaches used to combat guinea worm disease. This study seeks to provide a current and evidence-based summary of available treatment techniques by conducting an exhaustive examination of peer-reviewed literature, medical databases, and official health organisation publications.

Recent progress in nanomaterial-based aptamers as biosensors for point of care detection of Hg ions and its environmental applications.

Among the foremost persistent heavy metal ions in the ecosystem, mercury (Hg) remains intimidating to the environment by producing a catastrophic effect on the environment as well as on mankind due to the exacerbation of anthropogenic activities. Therefore, it has become necessary to develop superlative techniques for its detection even at low concentrations. The conventional approaches for Hg ions are quite laborious, and expensive, and require expertise in operating sophisticated instruments.

Recent Advancements and Future Prospects in NBD-Based Fluorescent Chemosensors: Design Strategy, Sensing Mechanism, and Biological Applications.

In recent years, the field of Supramolecular Chemistry has witnessed tremendous progress owing to the development of versatile optical sensors for the detection of harmful biological analytes. Nitrobenzoxadiazole (NBD) is one such scaffold that has been exploited as fluorescent probes for selective recognition of harmful analytes and their optical imaging in various cell lines including HeLa, PC3, A549, SMMC-7721, MDA-MB-231, HepG2, MFC-7, etc. The NBD-derived molecular probes are majorly synthesized from the chloro derivative of NBD nucleophilic aromatic substitution.

The Phytochemical Tactics for Battling Antibiotic Resistance in Microbes: Secondary Metabolites and Nano Antibiotics Methods.

One of the most serious threats to human health is antibiotic resistance, which has left the world without effective antibiotics. While continuous research and inventions for new antibiotics are going on, especially those with new modes of action, it is unlikely that this alone would be sufficient to win the battle. Furthermore, it is also important to investigate additional approaches.

Magnetite-supported montmorillonite (K) (nanocat-Fe-Si-K): an efficient green catalyst for multicomponent synthesis of amidoalkyl naphthol.

Montmorillonite (K) loaded on magnetite silica-coated nanoparticles was made using simple co-precipitation methods. The prepared nanocat-Fe-Si-K was analyzed using some techniques including field emission-scanning electron microscopy (FE-SEM), inductive coupling plasma-optical emission spectroscopy (ICP-OES), X-ray diffraction (XRD), thermo-gravimetric analysis (TGA), Fourier transmission-infrared spectra (FT-IR), energy dispersive X-ray spectroscopy (EDS), and wavelength-dispersive spectroscopy (WDX). The catalytic activity of the synthesized nanocat-Fe-Si-K has been examined in one-pot multicomponent transformations for the synthesis of 1-amidoalkyl 2-naphthol derivatives under solvent-free conditions.

Sulphur Containing Heterocyclic Compounds as Anticancer Agents.

After cardiovascular disease, cancer is the most common cause of death worldwide. Due to their versatility, heterocyclic compounds play an important role in drug discovery. Medical remedies are constantly being discovered, especially for catastrophic disorders such as cancer.

Structure activity relationship (SAR) and anticancer activity of pyrrolidine derivatives: Recent developments and future prospects (A review).

Pyrrolidine molecules are a significant class of synthetic and natural plant metabolites, which show the diversity of pharmacological activities. An extensive variety of synthetic pyrrolidine compounds with numerous derivatization like spirooxindole, thiazole, metal complexes, coumarin, etc have revealed significant anticancer activity. Pyrrolidine molecules are found not only as potential anticancer candidates but also retain the lowest side effects.

Marine-derived Natural Products as Anticancer Agents.

Cancer is a deadly human disease on the rise due to changes in lifestyle, nutrition, and global warming. Cancer is characterized by uncontrolled, disordered, and undesired cell division. About 60% of cancer medicines approved by the FDA are made from natural ingredients.

DNA intercalators as anticancer agents.

Cancer is one of the most prevailing disease conditions, which occurs due to uncontrolled cell division either due to natural mutation to the genes or due to changes induced by physical, chemical, or biological carcinogens. According to WHO, it is the second leading cause of death worldwide and has reported 10 million deaths in 2020. Hence, there arises the need for better chemotherapies and DNA intercalators are one such emerging therapy for cancer.

Synthesis and photobiological applications of naphthalimide-benzothiazole conjugates: cytotoxicity and topoisomerase IIα inhibition.

Conjugates of naphthalimide, benzothiazole, and indole moieties are synthesized that show excellent cytotoxicity against A549 (lung), MCF7 (breast), and HeLa (cervix) cancer cell lines with IC values in the range of 0.14-8.59 μM.

Copper(I) and silver(I) complexes of anthraldehyde thiosemicarbazone: synthesis, structure elucidation, anti-tuberculosis/cytotoxic activity and interactions with DNA/HSA.

A reaction of copper(i) halides (X = I, Br, Cl) and silver(i) halides with 9-anthraldehyde thiosemicarbazone (9-Hanttsc, H1L) and triphenylphosphine produced halogen-bridged dinuclear complexes, [M2(μ2-X)2(η1-S-9-Hanttsc)2(Ph3P)2] (M = Cu, X = Cl, 1; Br, 2; I, 3; M = Ag, X = Cl, 4; Br, 5). A similar reaction of 9-anthraldehyde-N1-methyl thiosemicarbazone (9-Hanttsc-N1-Me, H2L) with Ph3P and silver(i) halides yielded sulfur-bridged dimers, [Ag2X2(μ2-S-9-Hanttsc-N1-Me)2(Ph3P)2] (X = Cl, 9; Br, 10), however with copper(i) halides insoluble compounds were formed, which upon the addition of one extra mole of Ph3P gave mononuclear complexes of the formula [CuX(η1-S-9-Hanttsc-N1-Me)(Ph3P)2] (X = Cl, 6; Br, 7; I, 8). All of the complexes have been characterized by elemental analysis, NMR (1H, 13C) spectroscopy and single crystal X-ray crystallography (2, 5, 6, and 9).

Dual-channel ratiometric recognition of Al and F ions through an ESIPT-ESICT signalling mechanism.

An optical probe 1 has been synthesized comprising naphthalimide unit conjugated with Schiff base, exhibiting excited state intramolecular proton transfer and intramolecular charge transfer as a potential sensor for Al and F ions using standard spectroscopic techniques. The probe 1 exhibited local and charge-transfer excitation at 340 nm and 460 nm, respectively. On excitation at 460 nm, probe 1 displayed two emission bands at 510 nm and 610 nm, accompanied by Stokes' shift of 50 nm and 150 nm, respectively.

Synthesis, cytotoxicity, pharmacokinetic profile, binding with DNA and BSA of new imidazo[1,2-a]pyrazine-benzo[d]imidazol-5-yl hybrids.

Novel derivatives possessing imidazo[1,2-a]pyrazine and 1H-benzo[d]imidazole scaffolds were synthesized using Suzuki-Miyaura cross-coupling reactions. In vitro anticancer activities against NCI-60 cancer cell panels were tested at 10 µM concentration. The best results were obtained from substitution of two 1-cyclohexyl-1H-benzo[d]imidazole groups present at C-6 and C-8 positions of imidazo[1,2-a]pyrazine (31).

Spectroscopy and molecular docking approach for investigation on the binding of nocodazole to human serum albumin.

The interaction between nocodazole (Nz) and human serum albumin (HSA) under controlled physiological condition (pH 7.4) is examined using absorption, emission, fluorescence lifetime (FLT) and circular dichroism (CD) spectroscopic techniques. The binding constant (order of 10 M) from UV-vis and fluorescence spectroscopy reveals a strong interaction between Nz and HSA.

Synthesis of naphthalimide-phenanthro[9,10-d]imidazole derivatives: In vitro evaluation, binding interaction with DNA and topoisomerase inhibition.

The synthesis and characterization of a series of naphthalimide and phenanthro[9,10-d]imidazole conjugate is described. These compounds are evaluated in vitro for their cytotoxicity towards 60 human cancer cell lines. Derivative 16 shows excellent cytotoxic activity against these cancer cell lines with the range of growth inhibition from -55.

Effective synthesis of benzimidazoles-imidazo[1,2-a]pyrazine conjugates: A comparative study of mono-and bis-benzimidazoles for antitumor activity.

A novel series of 6-substituted-8-(1-cyclohexyl-1H-benzo[d]imidazole-6-yl)imidazo[1,2-a]pyrazine and 6-substituted-8-(1-benzyl-1H-benzo[d]imidazole-6-yl)imidazo[1,2-a]pyrazine is first time synthesized and screen in vitro biological activity for 60 human cancer cell lines representing nine different cancer types. Derivatives 10 and 36 show antitumor activity for all tested cell lines, display comparable full panel mean-graph midpoint growth inhibition (MG_MID GI) values of 2.10 and 2.

Synthesis and in vitro evaluation of naphthalimide-benzimidazole conjugates as potential antitumor agents.

A series of novel naphthalimide-benzimidazoles was designed and synthesized for the first time and studied for their effect on antiproliferative activity. Some of these compounds possessed good antitumor activity towards the tested cancer cell lines. Noticeably, (diethylamino)ethyl 15 and (dimethylamino)ethyl 23 derivatives displayed superior antiproliferative activity towards human cancer cell lines with MG_MID GI50 values of 1.

Synthesis of 5-(4-(1H-phenanthro[9,10-d]imidazol-2-yl)benzylidene)thiazolidine-2,4-dione as promising DNA and serum albumin-binding agents and evaluation of antitumor activity.

A series of phenanthro[9,10-d]imidazole/oxazole and acenaphtho[1,2-d]imidazole with different aryl groups at C2-position has been synthesized. These compounds were in vitro evaluated for antitumor activity against a panel of 60 human cancer cell lines. Compound 8 exhibits higher cytotoxicity towards leukemia, colon, melanoma, renal, and breast cancer cell lines than the other evaluated cell panels and low toxicity against normal cell line Hek293.

Recent Advances and Developments of in vitro Evaluation of Heterocyclic Moieties on Cancer Cell Lines.

Besides worthy development in cancer therapy, cancer is still one of the leading causes of death, worldwide. The future burden of cancer will probably be even larger because people are adopting poor lifestyles with poor diet, frequently smoking and less physical activity. The effective anticancer drugs having efficacy and selectivity with low toxicity is still a challenge for the scientific fraternity.