Structure-based discovery of small molecule inhibitors of FKBP51-Hsp90 protein-protein interaction.

The heat shock protein 90 kDa (Hsp90) molecular chaperone machinery is responsible for the folding and activation of hundreds of important clients such as kinases, steroid hormone receptors, transcription factors, etc. This process is dynamically regulated in an ATP-dependent manner by Hsp90 co-chaperones including a group of tetratricopeptide (TPR) motif proteins that bind to the C-terminus of Hsp90. Among these TPR containing co-chaperones, FK506-binding protein 51 kDa (FKBP51) is reported to play an important role in stress-related pathologies, psychiatric disorders, Alzheimer's disease, and cancer, making FKBP51-Hsp90 interaction a potential therapeutic target. In this study, we report identification of potent and selective inhibitors of FKBP51-Hsp90 protein-protein interaction using a structure-based virtual screening approach. Upon in vitro evaluation, the identified hits show a considerable degree of selectivity towards FKBP51 over other TPR proteins, particularly for highly homologous FKBP52. Tyr355 of FKBP51 emerged as an important contributor to inhibitor's specificity. Additionally, we demonstrate the impact of these inhibitors on cellular energy metabolism, and neurite outgrowth, which are subjects of FKBP51 regulation. Overall, the results from this study highlight a novel pharmacological approach towards regulation of FKBP51 function and more generally, Hsp90 function via its interaction with TPR co-chaperones.

Insights on Strain-Substrate Interactions and Antioxidant and Anti-Bacterial Properties of the Velvet Foot Medicinal Mushroom Flammulina velutipes (Agaricomycetes).

To study the best substrate for the Indian subcontinent, four different substrates (sawdust + wheat bran, wheat straw + wheat bran + corn cobs, sawdust + corn cobs and wheat straw + wheat bran) were screened for six different Flammulina velutipes strains. The antioxidant and antibacterial properties were studied for these strains. In study it was found that the strain DMRX-767 and DMRX-768 were the most promising for yield and biological efficiency in all substrates and wheat straw + wheat bran being the best with respect to BE. To corroborate the findings, the best strain and best substrate trails were repeated. DMRX-767 and DMRX-768 were the most promising for yield and biological efficiency in all substrates, with wheat straw+wheat bran were again found the best. The methanolic extract of strain DMRX-166 showed highest antibacterial properties as highest inhibition is found for Bacillus subtilis and Pseudomonas syringae. However, DMRO-253 inhibited Ralstonia solanacearum and Xanthomonas campestris. DMRX-768 has the best scavenging ability followed by DMRO-253.

Protein kinase inhibitors in the management of cancer: therapeutic opportunities from natural compounds.

Kinase is an enzyme that helps in the phosphorylation of the targeted molecules and can affect their ability to react with other molecules. So, kinase influences metabolic reactions like cell signaling, secretory processes, transport of molecules, etc. The increased activity of certain kinases may cause various types of cancer, i.e. leukemia, glioblastoma, and neuroblastomas. So, the growth of particular cancer cells can be prevented by the inhibition of the kinase responsible for those cancers. Natural products are the key resources for the development of new drugs where approximately 60% of anti-tumor drugs are being developed with the same including specific kinase dwellers. This study comprised molecular interactions of various molecules (obtained from natural sources) as kinase inhibitors for the treatment of cancer. It is expected that by analyzing the skeleton behavior, the process of action, and the body-related activity of these organic products, new cancer-avoiding molecules can be developed.

Tissue-targeted and localized AAV5-DCN and AAV5-PEDF combination gene therapy abrogates corneal fibrosis and concurrent neovascularization in rabbit eyes in vivo.

PURPOSE: Corneal fibrosis and neovascularization (CNV) after ocular trauma impairs vision. This study tested therapeutic potential of tissue-targeted adeno-associated virus5 (AAV5) mediated decorin (DCN) and pigment epithelium-derived factor (PEDF) combination genes in vivo. METHODS: Corneal fibrosis and CNV were induced in New Zealand White rabbits via chemical trauma. Gene therapy in stroma was delivered 30-min after chemical-trauma via topical AAV5-DCN and AAV5-PEDF application using a cloning cylinder. Clinical eye examinations and multimodal imaging in live rabbits were performed periodically and corneal tissues were collected 9-day and 15-day post euthanasia. Histological, cellular, and molecular and apoptosis assays were used for efficacy, tolerability, and mechanistic studies. RESULTS: The AAV5-DCN and AAV5-PEDF combination gene therapy significantly reduced corneal fibrosis (p < 0.01 or p < 0.001) and CNV (p < 0.001) in therapy-given (chemical-trauma and AAV5-DCN + AAV5-PEDF) rabbit eyes compared to the no-therapy given eyes (chemical-trauma and AAV5-naked vector). Histopathological analyses demonstrated significantly reduced fibrotic α-smooth muscle actin and endothelial lectin expression in therapy-given corneas compared to no-therapy corneas on day-9 (p < 0.001) and day-15 (p < 0.001). Further, therapy-given corneas showed significantly increased Fas-ligand mRNA levels (p < 0.001) and apoptotic cell death in neovessels (p < 0.001) compared to no-therapy corneas. AAV5 delivered 2.69 × 107 copies of DCN and 2.31 × 107 copies of PEDF genes per µg of DNA. AAV5 vector and delivered DCN and PEDF genes found tolerable to the rabbit eyes and caused no significant toxicity to the cornea. CONCLUSION: The combination AAV5-DCN and AAV5-PEDF topical gene therapy effectively reduces corneal fibrosis and CNV with high tolerability in vivo in rabbits. Additional studies are warranted.

Laminin mimetic angiogenic and collagen peptide hydrogel for enhance dermal wound healing.

Laminins are essential in basement membrane architecture and critical in re-epithelialization and angiogenesis. These processes and collagen deposition are vital in skin wound healing. The role of angiogenic peptides in accelerating the wound-healing process has been known. The bioactive peptides could be a potential approach due to their similar effects as growth factors and inherent biocompatible and biodegradable nature with lower cost. They can also recognize ligand-receptor interaction and mimic the extracellular matrix. Here, we report novel angiogenic DYVRLAI, CDYVRLAI, angiogenic-collagen PGPIKVAV, and Ac-PGPIKVAV peptides conjugated sodium carboxymethyl cellulose hydrogel, which was designed from laminin. The designed peptide exhibits a better binding with the α3ß1, αvß3, and α5ß1 integrins and CXCR2 receptor, indicating their angiogenic and collagen binding efficiency. The peptides were evaluated to stimulate wound healing in full-thickness excision wounds in normal and diabetic mice (type II). They demonstrated their efficacy in terms of angiogenesis (CD31), re-epithelialization through regeneration of the epidermis (H&E), and collagen deposition (MT). The synthesized peptide hydrogel (DYVRLAI and CDYVRLAI) showed enhanced wound contraction up to 10.1 % and 12.3 % on day 7th compared to standard becaplermin gel (49 %) in a normal wound model. The encouraging results were also observed with the diabetic model, where these peptides showed a significant decrease of 5.20 and 5.17 % in wound size on day 10th compared to the commercial gel (9.27 %). These outcomes signify that the modified angiogenic peptide is a cost effective, novel peptide motif to promote dermal wound healing in both models.

Dyadic and Individual Variation in 24-Hour Heart Rates of Cancer Patients and Their Caregivers.

BACKGROUND: Twenty-four-hour heart rate (HR) integrates multiple physiological and psychological systems related to health and well-being, and can be continuously monitored in high temporal resolution over several days with wearable HR monitors. Using HR data from two independent datasets of cancer patients and their caregivers, we aimed to identify dyadic and individual patterns of 24 h HR variation and assess their relationship to demographic, environmental, psychological, and clinical variables of interest. METHODS: a novel regularized approach to high-dimensional canonical correlation analysis (CCA) was used to identify factors reflecting dyadic and individual variation in the 24 h (circadian) HR trajectories of 430 people in 215 dyads, then regression analysis was used to relate these patterns to explanatory variables. RESULTS: Four distinct factors of dyadic covariation in circadian HR were found, contributing approximately 7% to overall circadian HR variation. These factors, along with non-dyadic factors reflecting individual variation exhibited diverse and statistically robust patterns of association with explanatory variables of interest. CONCLUSIONS: Both dyadic and individual anomalies are present in the 24 h HR patterns of cancer patients and their caregivers. These patterns are largely synchronous, and their presence robustly associates with multiple explanatory variables. One notable finding is that higher mood scores in cancer patients correspond to an earlier HR nadir in the morning and higher HR during the afternoon.

1,3,4-Oxadiazoles as Anticancer Agents: A Review.

Among the deadliest diseases, cancer is characterized by tumors or an increased number of a specific type of cell because of uncontrolled divisions during mitosis. Researchers in the current era concentrated on the development of highly selective anticancer medications due to the substantial toxicities of conventional cytotoxic drugs. Several marketed drug molecules have provided resistance against cancer through interaction with certain targets/growth factors/enzymes, such as Telomerase, Histone Deacetylase (HDAC), Methionine Aminopeptidase (MetAP II), Thymidylate Synthase (TS), Glycogen Synthase Kinase-3 (GSK), Epidermal Growth Factor (EGF), Vascular Endothelial Growth Factor (VEGF), Focal Adhesion Kinase (FAK), STAT3, Thymidine phosphorylase, and Alkaline phosphatase. The molecular structure of these drug molecules contains various heterocyclic moieties that act as pharmacophores. Recently, 1,3,4- oxadiazole (five-membered heterocyclic moiety) and its derivatives attracted researchers as these have been reported with a wide range of pharmacological activities, including anti-cancer. 1,3,4- oxadiazoles have exhibited anti-cancer potential via acting on any of the above targets. The presented study highlights the synthesis of anti-cancer 1,3,4-oxadiazoles, their mechanism of interactions with targets, along with structure-activity relationship concerning anti-cancer potential.

Glutathione Depletion and Concomitant Elevation of Susceptibility in Patients with Parkinson's Disease: State-of-the-Art MR Spectroscopy and Neuropsychological Study.

Parkinson's disease (PD) is characterized by extrapyramidal motor disturbances and nonmotor cognitive impairments which impact activities of daily living. Although the etiology of PD is still obscure, autopsy reports suggest that oxidative stress (OS) is one of the important factors in the pathophysiology of PD. In the current study, we have investigated the impact of OS in PD by measuring the antioxidant glutathione (GSH) levels from the substantia nigra (SN), left hippocampus (LH) and neurotransmitter γ-amino butyric acid (GABA) levels from SN region. Concomitant quantitative susceptibility mapping (QSM) from SN and LH was also acquired from thirty-eight PD patients and 30 age-matched healthy controls (HC). Glutathione levels in the SN region decreased significantly and susceptibility increased significantly in PD compared to HC. Nonsignificant depletion of GABA was observed in the SN region. GSH levels in the LH region were depleted significantly, but LH susceptibility did not alter in the PD cohort compared to HC. Neuropsychological and physical assessment demonstrated significant impairment of cognitive functioning in PD patients compared to HC. GSH depletion was negatively correlated to motor function performance. Multivariate receiver operating characteristic (ROC) curve analysis on the combined effect of GSH, GABA, and susceptibility in the SN region yielded an improved diagnostic accuracy of 86.1% compared to individual diagnostic accuracy based on GSH (65.8%), GABA (57.5%), and susceptibility (69.6%). This is the first comprehensive report in PD demonstrating significant GSH depletion as well as concomitant iron enhancement in the SN region.

Differential gene expression and protein-protein interaction network profiling of sulfur mustard-exposed rabbit corneas employing RNA-seq data and bioinformatics tools.

Sulfur mustard (SM) ocular exposure severely damages the cornea and causes vision impairment. At present, no specific therapy exists to mitigate SM-induced corneal injury and vision loss. This study performed transcriptome profiling of naïve, SM-damaged, and SM-undamaged rabbit corneas using RNA-seq analysis and bioinformatic tools to gain a better mechanistic understanding and develop SM-specific medical countermeasures. The mRNA profiles of rabbit corneas 4 weeks post SM vapor exposure were generated using Illumina-NextSeq deep sequencing (Gene Expression Omnibus accession # GSE127708). The RNA sequences of naïve (n = 4), SM-damaged (n = 5), and SM-undamaged (n = 5) corneas were subjected to differential expression (DE) analysis after quality control profiling with FastQC. DE analysis was performed using HISAT2, StringTie, and DESeq2. The log2(FC)±2 and adjusted p˂0.05 were chosen to identify the most relevant genes. A total of 5930 differentially expressed genes (DEGs) (upregulated: 3196, downregulated: 2734) were found in SM-damaged corneas compared to naïve corneas, whereas SM-undamaged corneas showed 1884 DEGs (upregulated: 1029, downregulated: 855) compared to naïve corneas. DE profiling of SM-damaged corneas to SM-undamaged corneas revealed 985 genes (upregulated: 308, downregulated: 677). The DE profiles were subsequently subjected to signaling pathway enrichment, and protein‒protein interactions (PPIs) were analyzed. Pathway enrichment was performed for the genes associated with cellular apoptosis, death, adhesion, migration, differentiation, proliferation, extracellular matrix, and tumor necrosis factor production. To identify novel targets, we narrowed the pathway analysis to upregulated and downregulated genes associated with cell proliferation and differentiation, and PPI networks were developed. Furthermore, protein targets associated with cell differentiation and proliferation that may play vital roles in corneal fibrosis and wound healing post SM injury were identified.

An Updated Review Summarizing the Anticancer Efficacy of Melittin from Bee Venom in Several Models of Human Cancers.

Apitherapy (using bee products) has gained broad recognition in cancer therapeutics globally. Honeybee venom has a broad range of biological potential, and its utilization is rapidly emerging in apitherapy. Bee products have significant potential to strengthen the immune system and improve human health. Thus, this review is targeted toward recapitulating the chemo-preventive potential of melittin (MEL), which constitutes a substantial portion of honeybee venom. Honeybee venom (apitoxin) is produced in the venom gland of the honeybee abdomen, and adult bees utilize it as a primary colony defense mechanism. Apitoxin comprises numerous biologically active compounds, including peptides, enzymes, amines, amino acids, phospholipids, minerals, carbohydrates, and volatile components. We are mainly focused on exploring the potential of melittin (a peptide component) of bee venom that has shown promising potential in the treatment of several human cancers, including breast, stomach, lung, prostate, ovary, kidney, colon, gastric, esophageal, cervical cancers, melanoma, osteosarcoma, and hepatocellular carcinoma. This review has summarized all potential studies related to the anticancerous efficacy of melittin (apitoxin), its formulations, conjugates, and nano-formulations against several human carcinomas, which would further pave the way for future researchers in developing potent drugs for cancer management.

Deep learning-based prediction model for diagnosing gastrointestinal diseases using endoscopy images.

BACKGROUND: Gastrointestinal (GI) infections are quite common today around the world. Colonoscopy or wireless capsule endoscopy (WCE) are noninvasive methods for examining the whole GI tract for abnormalities. Nevertheless, it requires a great deal of time and effort for doctors to visualize a large number of images, and diagnosis is prone to human error. As a result, developing automated artificial intelligence (AI) based GI disease diagnosis methods is a crucial and emerging research area. AI-based prediction models may lead to improvements in the early diagnosis of gastrointestinal disorders, assessing severity, and healthcare systems for the benefit of patients as well as clinicians. The focus of this research is on the early diagnosis of gastrointestinal diseases using a convolution neural network (CNN) to enhance diagnosis accuracy. METHODS: Various CNN models (baseline model and using transfer learning (VGG16, InceptionV3, and ResNet50)) were trained on a benchmark image dataset, KVASIR, containing images from inside the GI tract using n-fold cross-validation. The dataset comprises images of three disease states-polyps, ulcerative colitis, and esophagitis-as well as images of the healthy colon. Data augmentation strategies together with statistical measures were used to improve and evaluate the model's performance. Additionally, the test set comprising 1200 images was used to evaluate the model's accuracy and robustness. RESULTS: The CNN model using the weights of the ResNet50 pre-trained model achieved the highest average accuracy of approximately 99.80% on the training set (100% precision and approximately 99% recall) and accuracies of 99.50% and 99.16% on the validation and additional test set, respectively, while diagnosing GI diseases. When compared to other existing systems, the proposed ResNet50 model outperforms them all. CONCLUSION: The findings of this study indicate that AI-based prediction models using CNNs, specifically ResNet50, can improve diagnostic accuracy for detecting gastrointestinal polyps, ulcerative colitis, and esophagitis. The prediction model is available at https://github.com/anjus02/GI-disease-classification.git.

Synthetic approaches and applications of an underprivileged 1,2,5-oxadiazole moiety: A review.

1,2,5-oxadiazole belongs to five-membered heterocyclic compounds with two nitrogen and one oxygen atom. In comparison with other heterocyclic moieties, 1,2,5-oxadiazoles moiety is considered as underprivileged as it attracted little attention of the researchers although lot of scopes and possible applications in medicinal, material and agriculture science. 1,2,5-oxadiazole and its derivatives have been reported as good pharmacophores as carbonic anhydrase inhibitors, antibacterial, vasodilating agents, antimalarial, anticancer, etc. In the presented manuscript, we reviewed granted patents and different synthetic strategies which have been reported for the synthesis of 1,2,5-oxadiazoles such as cycloaddition, dimerization, cyclodehydration, condensation, thermolysis, nitration, oxidation and ring-conversion. These synthetic methods have also been analysed for their merits and demerits. The manuscript also highlighted various applications of 1,2,5-oxadiazole and its derivatives. We hope that researchers across the scientific streams will be benefitted from the presented review articles for designing their work related to 1,2,5-oxadiazoles.

Artificial intelligence in intestinal polyp and colorectal cancer prediction.

Artificial intelligence (AI) algorithms and their application to disease detection and decision support for healthcare professions have greatly evolved in the recent decade. AI has been widely applied and explored in gastroenterology for endoscopic analysis to diagnose intestinal cancers, premalignant polyps, gastrointestinal inflammatory lesions, and bleeding. Patients' responses to treatments and prognoses have both been predicted using AI by combining multiple algorithms. In this review, we explored the recent applications of AI algorithms in the identification and characterization of intestinal polyps and colorectal cancer predictions. AI-based prediction models have the potential to help medical practitioners diagnose, establish prognoses, and find accurate conclusions for the treatment of patients. With the understanding that rigorous validation of AI approaches using randomized controlled studies is solicited before widespread clinical use by health authorities, the article also discusses the limitations and challenges associated with deploying AI systems to diagnose intestinal malignancies and premalignant lesions.

Corneal gene therapy: Structural and mechanistic understanding.

Cornea, a dome-shaped and transparent front part of the eye, affords 2/3rd refraction and barrier functions. Globally, corneal diseases are the leading cause of vision impairment. Loss of corneal function including opacification involve the complex crosstalk and perturbation between a variety of cytokines, chemokines and growth factors generated by corneal keratocytes, epithelial cells, lacrimal tissues, nerves, and immune cells. Conventional small-molecule drugs can treat mild-to-moderate traumatic corneal pathology but requires frequent application and often fails to treat severe pathologies. The corneal transplant surgery is a standard of care to restore vision in patients. However, declining availability and rising demand of donor corneas are major concerns to maintain ophthalmic care. Thus, the development of efficient and safe nonsurgical methods to cure corneal disorders and restore vision in vivo is highly desired. Gene-based therapy has huge potential to cure corneal blindness. To achieve a nonimmunogenic, safe and sustained therapeutic response, the selection of a relevant genes, gene editing methods and suitable delivery vectors are vital. This article describes corneal structural and functional features, mechanistic understanding of gene therapy vectors, gene editing methods, gene delivery tools, and status of gene therapy for treating corneal disorders, diseases, and genetic dystrophies.

Synthesis and SAR of Potential Anti-Cancer Agents of Quinoline Analogues: A Review.

Quinoline has recently become an important heterocyclic molecule due to its numerous industrial and synthetic organic chemistry applications. Quinoline derivatives have been used in clinical trials for a variety of medical conditions that causes cancer. The present literature study is composed of recent progress (mainly from 2010 to the present) in the production of novel quinoline derivatives as potential anti-cancer agents, as well as their structure-activity relationship, which will provide insight into the development of more active quinoline hybrids in the future. The present review comprises the synthetic protocols of biologically active Quinoline analogs with their structure-activity relationship studies as anti-cancer agents, which provide depth view of work done on quinoline derivatives to the medicinal chemist for future research.

Design of CO2 Thickeners and Role of Aromatic Rings in Enhanced Oil Recovery Using Molecular Dynamics.

Oligomers of PDMS (M1), polyFast (M2), modified PVEE (M3 and M4), and two new molecules with cyclic cores (M5 and M6) were studied to understand their ability to thicken the sc-CO2 at 377 K and 55 MPa, without any cosolvent. It was observed that PDMS and polyFast behaved in the known ways. PDMS does not improve the viscosity of the system without a cosolvent and PolyFast enhances the viscosity by a large margin. M3 and M4 also have not improved the viscosity significantly even with the introduction of a styrene component, but which has improved their solubilities in the fluid. M5 and M6, however, are observed to have enhanced the viscosity similar to that of polyFast due to their structural advantage and π-π interactions between the molecules. These molecules were also tested for their synthesizability, and their synthesis is found to be moderately easy.

Synthesis, biological evaluation and in silico studies of 2-aminoquinolines and 1-aminoisoquinolines as antimicrobial agents.

The current study reports synthesis of 2-aminoquinolines and 1-aminoisoquinolines derivatives and their characterization. Further, in vitro studies were conducted to determine antimicrobial activities. Compound 3 h showed maximum activity against B. subtilis (IC50: 0.10±0.02 µM) and E. coli (IC50: 0.13±0.01 µM) whereas compound 3i showed higher antimicrobial activity against E. coli (IC50: 0.11±0.01) and C. viswanathii (IC50: 0.10±0.05 µM). Safety profiles of the most potent derivatives were evaluated utilizing cell viability assay using RAW 264.7 and HeLa cell lines and in vitro hemolytic assay was carried out freshly isolated RBC from healthy rat. Furthermore, in silico studies, like molecular docking, binding free energy calculations and ADME predictions were done to get the best lead candidates. Additionally, molecular dynamic simulation for 100 ns was performed to know stability of protein and ligand complex. The active compounds were found to be non-toxic and non-hemolytic and hold great promise to become newer antimicrobial agents.

Epigenetic Modifications by Estrogen and Androgen in Alzheimer's Disease.

For the development and maintenance of neuron networks in the brain, epigenetic mechanisms are necessary, as indicated by recent findings. This includes some of the high-order brain processes, such as behavior and cognitive functions. Epigenetic mechanisms could influence the pathophysiology or etiology of some neuronal diseases, altering disease susceptibility and therapy responses. Recent studies support epigenetic dysfunctions in neurodegenerative and psychiatric conditions, such as Alzheimer's disease (AD). These dysfunctions in epigenetic mechanisms also play crucial roles in the transgenerational effects of the environment on the brain and subsequently in the inheritance of pathologies. The possible role of gonadal steroids in the etiology and progression of neurodegenerative diseases, including Alzheimer's disease, has become the subject of a growing body of research over the last 20 years. Recent scientific findings suggest that epigenetic changes, driven by estrogen and androgens, play a vital role in brain functioning. Therefore, exploring the role of estrogen and androgen-based epigenetic changes in the brain is critical for the deeper understanding of AD. This review highlights the epigenetic modifications caused by these two gonadal steroids and the possible therapeutic strategies for AD.

Recent Updates on Synthesis, Biological Activity, and Structure-activity Relationship of 1,3,4-Oxadiazole-quinoline Hybrids: A Review.

Due to their diverse applications in industrial and synthetic organic chemistry, quinoline and 1,3,4-oxadiazole have become important heterocyclic compounds. Quinoline and 1,3,4- oxadiazole compounds have been developed for various medical conditions such as anti-cancer, anti-bacterial, anti-fungal, antimalarial, antioxidants, anti-HIV, anticonvulsant, antiviral, etc. The current review includes synthetic protocols for biologically active 1,3,4-oxadiazole incorporating quinoline hybrids with their structure-activity relationship to explore work (Mainly from 2010 to 2021) based on 1,3,4-oxadiazole-quinoline hybrids to the medicinal chemist for further research in the development of the molecule.

Camphor and Menthol as Anticancer Agents: Synthesis, Structure-Activity Relationship and Interaction with Cancer Cell Lines.

Cancer is a type of human cell degenerative disease that has afflicted a large number of people for years. Cancer is caused due to the abnormal proliferation of cells in any part of the body. Most of the prescribed anticancer drugs are synthetic in nature and have been reported with enormous adverse effects. The researchers are very much enthusiastic about the use of natural compounds and their derivatives, which have been reported with less toxicity. Natural compounds have emerged as promising synergistic compounds with potential anticancer effects. In vitro anticancer activity of natural compounds with special reference to camphor and menthol has been investigated against different cancer cell lines. It has been found that camphor and menthol derivatives have potential cytotoxic activity. The present literature review outlines the various methods for the synthesis of camphor and menthol derivatives, which have potential cytotoxic activity. It highlights various cancer cell lines, which are the target of these camphor and menthol derivatives as ligands, along with structure-activity studies.