Characterization, Antioxidant, and Antimicrobial Properties of Mulberry Lattices.

In order to find the most advantageous bioactive compounds from mulberry latex for drug development in the near future, this study was conducted to characterize and evaluate antioxidant and antimicrobial properties from four different mulberry lattices (BR-2, S-1, AR-14, and S-146). The characterization of the lattices was performed by scanning electron microscopy with energy-dispersive X-ray spectroscopy, gas chromatography coupled to mass spectroscopy, and Fourier transform infrared spectroscopy. Further, screenings of the antioxidant and antimicrobial potential of selected lattices were performed in vitro using 2,2-diphenyl-1-picrylhydrazyl assay and agar well diffusion methods, respectively. Interestingly, the outcome of the current study revealed that tested mulberry lattices contain a considerable amount of bioactive phytoconstituents, particularly antimicrobial and antioxidant compounds, as revealed by chromatographic analysis. BR-2 latex was found to have significant antioxidant activity (75%) followed by S-146 (64.6%) and AR-14 (52.9%). The maximum antimicrobial activity was found in BR-2 latex compared to other tested latex varieties. The results of this investigation showed that mulberry latex from the BR-2 type may successfully control both bacterial and fungal infections, with the added benefit of having enhanced antioxidant capabilities.

Trophic functioning of a small, anthropogenically disturbed, tropical estuary.

A trophic model was constructed for the Poonthura Estuary, a small, anthropogenically impacted estuary along the south-western coast of India. An Ecopath with Ecosim based trophic modelling approach, based on observations made between 2016 and 2020, revealed that the Poonthura Estuary had a low total system throughput (3044.2 t km-2 year-1), low ascendancy (15%), high Finn's cycling index (17.9%), low primary production/total biomass (5.2 t km-2 year-1), high mean transfer efficiency (12.4%), and low eco-exergy (14,455.46 gm detritus equivalent m-2). These values indicated that the estuary is an immature, less organized, and unhealthy system. The evaluation of Ecological Network Analysis, and ecosystem health indices revealed that the ecological structure and functioning of the estuary are impaired to a large extent from multiple anthropogenic stressors. The Poonthura Estuary trophic model revealed the total primary production/respiration value as 0.46, indicative of the massive pollution that the system is subjected to, particularly from organic sources. Small benthic carnivores were the most important keystone groups recorded from the Poonthura Estuary, despite their low biomass. The comparison of ecological indices of Poonthura Estuary, with those recorded for other small estuaries from various geographical locations, suggested dissimilar trophic functioning and food web structures from estuaries with similar physical features. Our study is a pioneering step to reveal the ecosystem status and functioning of small, anthropogenically disturbed estuaries, besides offering theoretical and scientific basis for the management, supervision and restoration of the Poonthura Estuary as well as other small estuaries, around the world.

Combined Radiological and Endoscopic Evaluation of Sino Nasal Anatomical Variations in Patients of Chronic Rhinosinusitis: A North Indian Study.

To determine the prevalence of anatomical variations of nasal cavity and paranasal sinuses of patients with chronic rhinosinusitis (CRS) on CT scan imaging. To correlate the Anatomical variations with the extent of CRS. 100 patients attending the ENT outpatient department with clinically diagnosed CRS were selected for study based on inclusion and exclusion criteria. Patients were subjected to CT scan and diagnostic nasal endoscopy. The correlation of anatomical variation with severity of CRS based on radiological score and endoscopic score was observed. Deviated nasal septum was the most common anatomical variation observed in 71% cases. Followed by Agger nasi (68%), concha bullosa (55%), Onodi cell (25%), Haller cell (14%), frontal sinus hypoplasia (2%) and uncinate bulla (1%) respectively. Statistically significant relationship of radiological score with left side Bullous Concha Bullosa and highly statistically significant relationship with Haller Cell was observed. While statistically significant relationship between Deviated Nasal Septum on left side with endoscopic score was also observed. Correlation of anatomical variation with CRS concludes on the note that some variations cause impaired sinus drainage and ventilation leading to recurrent sinusitis. Also, incidence of these variations was comparable to other studies done in asymptomatic population therefore, simply detection of a solitary anatomical variant itself does not determine predisposition to disease or the pathogenesis of the CRS and that we should have a critical look out for these anatomical variations from point of view of surgical management.

Design, synthesis and biological evaluation of phenanthridine amide and 1,2,3-triazole analogues against Mycobacterium tuberculosis.

The phenanthridine core exhibits antitubercular activity, according to reports from the literature. Several 1,2,3-triazole-based heterocyclic compounds are well-known antitubercular agents. A series of twenty-five phenanthridine amide and 1,2,3-triazole derivatives are synthesized and analyzed using ESI-MS, 1HNMR, and 13CNMR on the basis of our earlier findings that phenanthridine and 1,2,3-triazoles shown good antitubercular activity. The synthesized phenanthridine amide and 1,2,3-triazole analogues were tested in vitro against Mycobacterium tuberculosis H37Rv and minimum inhibitory concentration (MIC) values were determined utilizing non-replicating and replicating low-oxygen recovery assay (LORA) and microplate Alamar Blue assay (MABA) methodologies. The phenanthridine amide derivative PA-01 had an MIC of 61.31 µM in MABA and 62.09 µM in the LORA technique, showing intense anti-TB activity. Amongst the phenanthridine triazole derivatives, PT-09, with MICs of 41.47 and 78.75 µM against the tested strain of Mtb in both MABA and LORA was the most active one. The final analogues' drug-likeness is predicted using absorption, distribution, metabolism, excretion, and toxicity (ADMET) studies. The most active compounds PA-01 and PT-09 were further subjected to in silico docking studies. Using the Glide module of Schrodinger, molecular docking analysis was carried out to estimate the plausible binding pattern of PA-01 and PT-09 at the active site of Mycobacterial DNA topoisomerase II (PDB code: 5BS8). Further, molecular dynamics studies of PA-01 and PT-09 were also carried out.

Neurofibrolipoma of Hypopharynx: A Rare Entity.

A Large pedunculated neurofibrolipoma involving the hypopharynx is a very rare entity. Patient with hypopharyngeal polyp usually presents with progressive dyaphagia, sensation of persistent lump in throat and difficulty in breathing. Regurgitation of the mass into the airway can led to fatal asphyxiation on several occasions and may rarely cause death also if not evaluated and treated timely. Malignant degeneration of these large polyps occurs infrequently. We encountered a case with similar complaints in our outpatient department. After complete clinical examination, radiological investigations and anaesthetic evaluation; patient was taken for elective tracheostomy first and subsequently followed by successful transoral endoscopic excision of hypopharyngeal polypoidal mass. The histopathological examination of mass revealed it to be a neurofibrolipoma.

Molecular-level strategic goals and repressors in Leishmaniasis - Integrated data to accelerate target-based heterocyclic scaffolds.

Leishmaniasis is a complex of neglected tropical diseases caused by various species of leishmanial parasites that primarily affect the world's poorest people. A limited number of standard medications are available for this disease that has been used for several decades, these drugs have many drawbacks such as resistance, higher cost, and patient compliance, making it difficult to reach the poor. The search for novel chemical entities to treat leishmaniasis has led to target-based scaffold research. Among several identified potential molecular targets, enzymes involved in the purine salvage pathway include polyamine biosynthetic process, such as arginase, ornithine decarboxylase, S-adenosylmethionine decarboxylase, spermidine synthase, trypanothione reductase as well as enzymes in the DNA cell cycle, such as DNA topoisomerases I and II plays vital role in the life cycle survival of leishmanial parasite. This review mainly focuses on various heterocyclic scaffolds, and their specific inhibitory targets against leishmaniasis, particularly those from the polyamine biosynthesis pathway and DNA topoisomerases with estimated activity studies of various heterocyclic analogs in terms of their IC50 or EC50 value, reported molecular docking analysis from available published literatures.

EVALUATION OF ACCURACY AND INTRINSIC UNCERTAINTY OF AUTOMATED IMAGE REGISTRATION FOR A 6D KV-CBCT IMAGE GUIDANCE SYSTEM: A CONCURRENT ANALYSIS WITH A MACHINE PERFORMANCE CHECK.

The accuracy and uncertainty of the automated image registration (AIR) algorithm in a six-dimensional (6D) kilovoltage cone-beam computed tomography (kV-CBCT) image-guided radiation therapy (IGRT) system were evaluated with a concurrent analysis of machine performance check (MPC). The MPC was performed before (MPCpre) and after (MPCpost) each accuracy and intrinsic uncertainty measurement. The accuracy was evaluated for 25 sets of the known shifts applied to the Catphan-504 phantom through a 6D robotic couch in the head, thorax, and pelvis CBCT acquisition modes. The uncertainty was evaluated for the intensity range, soft tissue, and bone matching filters in the head, thorax and pelvis CBCT acquisition modes. The mean ΔMPC (MPCpost-MPCpre) for all test parameters was within 0.02 ± 0.08 mm and 0.00 ± 0.02°. The overall average accuracy in AIR of 6D kV-CBCT IGRT in all translational and rotational axes was within 0.05 ± 0.76 mm and 0.02 ± 0.07°, respectively, for all CBCT modes. The overall mean population (Mpop), systematic (Σ) and random (σ) errors were within 0.47, 0.53 and 0.24 mm and within 0.03, 0.08 and 0.07° in translational and rotational axes, respectively, for all matching filters in all CBCT modes. The accuracy and intrinsic uncertainty in the AIR of the 6D kV-CBCT IGRT were within acceptable limits for clinical use.

Retrospective Review of Chromane Analogues as Anti-protozoal Leads: A Decade's Worth of Evolution.

Tropical, vector-borne, and neglected diseases with a limited number of medication therapies include Leishmaniasis, Malaria, Chagas and Human African Trypanosomiasis (HAT). Chromones are a large class of heterocyclic compounds with significant applications. This heterocycle has long aroused the interest of scientists and the general public from biosynthetic and synthetic points of view owing to its interesting pharmacological activities. Chromones and their hybrids and isomeric forms proved to be an exciting scaffold to investigate these diseases. The in vitro activities of Chromone, Chromane, and a panel of other related benzopyran class compounds against Trypanosoma brucei rhodesiense, Trypanosoma brucei gambiense, Trypanosoma cruzi, and numerous Leishmanial and Malarial species were investigated in our previous studies. The current article briefly describes the neglected diseases and the current treatment. This review aims to attempt to find better alternatives by scrutinizing natural and synthetic derivatives for which chromones and their analogues were discovered to be a new and highly effective scaffold for the treatment of neglected diseases, including compounds with dual activity or activity against multiple parasites. Additionally, the efficacy of other new scaffolds was also thoroughly examined. This article also discusses prospects for identifying more unique targets for the disease, focusing on flavonoids as drug molecules that are less cytotoxic and high antiprotozoal potential. It also emphasizes the changes that can be made while searching for potential therapies-comparing existing treatments against protozoal diseases and the advantages of the newer chromone analogues over them. Finally, the structure- activity relationship at each atom of the chromone has also been highlighted.

QUANTIFICATION OF 6D INTER-FRACTION TUMOUR LOCALISATION ERRORS IN TONGUE AND PROSTATE CANCER USING DAILY KV-CBCT FOR 1000 IMRT AND VMAT TREATMENT FRACTIONS.

This study aimed to evaluate the 6D inter-fraction tumour localisation errors in 20 tongue and 20 prostate cancer patients treated with intensity-modulated radiation therapy and volumetric-modulated arc therapy. The patient tumour localisation errors in lateral, longitudinal and vertical translation axes and pitch, roll and yaw rotational axes were analysed by automatic image registration of daily pretreatment kilovoltage cone-beam computed tomography (kV-CBCT) with planning CT in 1000 fractions. The overall mean error (M), systematic error (Σ), random error (σ) and planning target volume (PTV) margins were evaluated. The frequency distributions of setup errors were normally distributed about the mean except for pitch in the tongue and prostate. The overall 3D vector length ≥ 5 mm was 14.2 and 49.8% in the ca-tongue and ca-prostate, respectively. The frequency of rotational errors ≥1 degree was a maximum of 37 and 59.5%, respectively, in ca-tongue and ca-prostate. The M, Σ and σ for all translational and rotational axes decreased with increasing frequency of verification correction in ca-tongue and ca-prostate patients. Similarly, the PTV margin was reduced with no correction to alternate day correction from a maximum of 4.7 to 2.5 mm in ca-tongue and from a maximum of 8.6 to 4.7 mm in ca-prostate. The results emphasised the vital role of the higher frequency of kV-CBCT based setup correction in reducing M, Σ, σ and PTV margins in ca-tongue and ca-prostate patients.

Design, synthesis and evaluation of novel phenanthridine triazole analogs as potential antileishmanial agents.

Aim: To synthesize and screen phenanthridine and 1,2,3-triazole derivatives for antileishmanial activity. Methodology: Synthesized analogs were tested for antileishmanial activity against transgenic strain of Leishmania infantum promastigotes and ex vivo infections. Results: Compounds T01, T08 and T11 revealed significant activity with EC50 <30 µm and lacked toxicity in mouse spleen and HepG2 cells. T01 with EC50 3.07 µm is fourfold more potent than the drug miltefosine (EC50 12.6 µM) against L. infantum promastigotes. In silico studies indicate that the analogs are nontoxic. A molecular docking analysis was also carried out on the T01 and T08 to investigate the binding pattern at the active site of the chosen target trypanothione reductase. Conclusion: The results of this study reveal that phenanthridine triazoles exhibit antileishmanial activity.

Design, synthesis and anti-mycobacterial evaluation of imidazo[1,2-a]pyridine analogues.

Based on the molecular hybridization strategy, thirty-four imidazo[1,2-a]pyridine amides (IPAs) and imidazo[1,2-a]pyridine sulfonamides (IPSs) were designed and synthesized. The structures of the target compounds were characterized using 1H NMR, 13C NMR, LCMS, and elemental analyses. The synthesized compounds were evaluated in vitro for anti-tubercular activity using the microplate Alamar Blue assay against Mycobacterium tuberculosis H37Rv strain and the MIC was determined. The evaluated compounds exhibited MIC in the range 0.05-≤100 µg mL-1. Among these derivatives, IPA-6 (MIC 0.05 µg mL-1), IPA-9 (MIC 0.4 µg mL-1), and IPS-1 (MIC 0.4 µg mL-1) displayed excellent anti-TB activity, whereas compounds IPA-5, IPA-7 and IPS-16 showed good anti-TB activity (MIC 0.8-3.12 µg mL-1). The most active compounds with MIC of <3.125 µg mL-1 were screened against human embryonic kidney cells to check their cytotoxicity to normal cells. It was observed that these compounds were nontoxic (SI value ≥66). The ADMET characteristics of the final compounds were also predicted in silico. Further, using the Glide module of Schrodinger software, a molecular docking study of IPA-6 was carried out to estimate the binding pattern at the active site of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis (PDB 4TZK). Finally, molecular dynamics simulations were performed for 100 ns to elucidate the stability, conformation, and intermolecular interactions of the co-crystal ligand and significantly active compound IPA-6 on the selected target protein. IPA-6, the most active compound, was found to be 125 times more potent than the standard drug ethambutol (MIC 6.25 µg mL-1).

Discovery of potent antitubercular agents: Design, synthesis and biological evaluation of 4-(3-(4-substitutedpiperazin-1-yl)-quinoxalin-2-yl)-naphthalen-1-ol analogues.

A series of twenty-five novel 4-(3-(4-substituted piperazin-1-yl)-quinoxalin-2-yl)-naphthalen-1-ol analogues were synthesized, characterized and screened for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain. These compounds exhibited minimum inhibitory concentration in the range of 1.56-50 µg/mL. Among these derivatives, compounds 5a, 5b, 5f, 5m, 5p, and 5r displayed moderate activity (MIC 6.25 µg/mL). Compounds 5c, 5d, 5g, 5l, and 5o showed significant antitubercular activity (MIC 3.125 µg/mL), while compounds 5h, 5n, and 5q exhibited potent antitubercular activity (MIC 1.56 µg/mL). In addition, MTT assay was performed on the active analogues of the series against mouse macrophage cells to assess the cytotoxic effect of the newly synthesized compounds, and a selectivity index of the compounds was established. Selectivity index values of the most active compounds (5h, 5n, and 5q) are >47, indicating the compounds' suitability for further potential drug development. A molecular docking study was performed to understand the putative binding mode and binding strength of the selected significantly active and weakly active compounds with the target enzyme mycobacterial topoisomerase II using moxifloxacin as standard. In-silico ADME prediction and bioavailability studies of the titled compounds obey Lipinski's rule of five and Jorgensen's rule of three. To further ascertain the structure of the compounds, a suitable single crystal for the compounds 5a, 6, and 7d was developed and studied.

Abundance and characteristics of microplastics in gastrointestinal tracts and gills of croaker fish (Johnius dussumieri) from off Mumbai coastal waters of India.

The present study was conducted to establish the intensity of microplastic pollution in demersal fish species, Johnius dussumieri, from the north eastern coastal waters of the Arabian sea. MP recovered were analysed for size, morphology, colour, and polymer type. The study results indicated that the GI tract and gills of individual fishes had 6.6 ± 1.7 and 6.2 ± 1.7 items, respectively. The microplastics having a size of <100 µm consisting of beads were found to be most predominant. Black and blue were the most present colours of microplastic in the tissues. Among the different studied months, a higher number of MP incidence was observed in the post monsoon period. There is no significant correlation observed between the microplastic numbers in gills and guts tissue. The present study shows that there is a potential risk of microplastic bioaccumulation in the fish body and subsequent risk to the consumers and organisms sharing the food chain.

Evaluation of kV-CBCT based 3D dose calculation accuracy and its validation using delivery fluence derived dose metrics in Head and Neck Cancer.

PURPOSE: The purpose of this study is to evaluate the dosimetric impact of Hounsfield unit (HU) variations in kilovoltage cone-beam computed tomography (kV-CBCT) based 3D dose calculation accuracy in the treatment planning system and its validation using measured treatment delivery dose (MTDD) derived dose metrics for Volumetric Modulated Arc Therapy (VMAT) and Intensity Modulated Radiotherapy (IMRT) plans in Head and Neck (HN) Cancer. METHODS: CBCT dose calculation accuracy was evaluated for 8 VMAT plans on inhomogeneous phantom and 40 VMAT and IMRT plans of HN Cancer patients and validated using ArcCHECK diode array MTDD derived 3D dose metric on CT and CBCT. RESULTS: The mean percentage dose difference between CBCT and CT in TPS (ΔD(CBCT-CT)TPS) and 3DVH (ΔD(CBCT-CT)3DVH) were compared for the corresponding evaluation dose metrics (D98%, D95%, D50%, D2%, Dmax, D1cc, D0.03cc, Dmean) of all PTVs and OARs in phantom and patients. ΔD(CBCT-CT)TPS and ΔD(CBCT-CT)3DVH for all evaluation dose points of all PTVs and OARs were less than 2.55% in phantom and 2.4% in HN patients. The Pearson correlation coefficient (r) between ΔD(CBCT-CT)TPS and ΔD(CBCT-CT)3DVH for all dose points in all PTVs and OARs showed a strong to moderate correlation in phantom and patients with p < 0.001. CONCLUSIONS: This study evaluated and validated the potential feasibility of kV-CBCT for treatment plan 3D dose reconstruction in clinical decision making for Adaptive radiotherapy on CT in Head and Neck cancer.

Design, synthesis and structure-activity relationship studies of novel spirochromanone hydrochloride analogs as anticancer agents.

Aim: Literature reports suggest spirochromanone derivatives exhibit anticancer activity. Methodology: The authors designed and synthesized 18 spirochromanone derivatives (Csp 1-18). The compounds were characterized and evaluated for anticancer activity against human breast cancer (MCF-7) and murine melanoma (B16F10) cell lines. Results: The anticancer activity ranged from 4.34 to 29.31 µm. The most potent compounds, Csp 12 and Csp 18, were less toxic against the human embryonic kidney (HEK-293) cell line and ∼ two/∼fourfold selective toward MCF-7 than B16F10 in comparison to the reference, BG-45. Csp 12 caused 28.6% total apoptosis, leading to significant cytotoxicity, and arrested the G2 phase of the cell cycle in B16F10 cells. A molecular docking study of Csp 12 exhibited effective binding at the active site of the epidermal growth factor receptor kinase domain. Conclusion: This study highlights the importance of spirochromanones as anticancer agents.

Design, synthesis and evaluation of novel ß-carboline ester analogues as potential anti-leishmanial agents.

Leishmaniasis is one of today's most neglected diseases. The emergence of new anti-leishmanial therapies emphasizes several study groups funded by the World Health Organization. The present investigation will focus on the research to determine a few new potential derivatives of ß-carboline ester derivatives against leishmaniasis. The in-silico predicted ADMET properties of most of the titled compounds are in an acceptable range and having drug like properties. Among all the tested analogs, compound ES-3 (EC50 3.36 µM; SI > 29.80) showed comparable and equipotent anti-leishmanial activity as that of standard drug miltefosine (EC50 4.80 µM; SI > 20.80) against amastigote forms of the tested L. infantum strain. Two compounds ES-6 and ES-10 exhibited significant activity with EC50 10.16, 13.56 µM; SI > 4.90, 7.37, respectively. In-silico based molecular docking and dynamics study of the significantly active analog also performed to study the putative binding mode, interaction pattern at the active site of the target leishmanial trypanothione reductase enzyme as well as stability of the target-ligand complex. The changes in the conformation of molecules during MD (frame wise trajectory analysis) provided new insights for the development of novel potent molecules. These findings will further give insight that will help modify the compound ES-3 for better potency and the design of novel inhibitors for leishmaniasis.Communicated by Ramaswamy H. Sarma.

Rare Case of C3 Glomerulopathy in a Patient of Type 1 Diabetes Mellitus.

Complement component 3 glomerulopathy (C3G) is a recently defined entity comprising dense deposit disease and C3 glomerulonephritis. It is associated with nonrenal diseases such as diabetes mellitus (DM) type 1, ocular drusen, acquired partial lipodystrophy, and monoclonal gammopathy of undetermined significance. We describe a case of 13-year-old boy of the known case of type 1 DM, who developed proteinuria, and swelling over his face, and lower limbs, which on renal biopsy, was diagnosed as a case of C3G.

Novel phenanthridine amide analogs as potential anti-leishmanial agents: In vitro and in silico insights.

In the current work, sixteen novel amide derivatives of phenanthridine were designed and synthesized using 9-fluorenone, 4-Methoxy benzyl amine, and alkyl/aryl acids. The characterization of the title compounds was performed using LCMS, elemental analysis, 1HNMR, 13CNMR and single crystal XRD pattern was also developed for compounds A8. All the final analogs were screened in vitro for anti-leishmanial activity against promastigote form of L. infantum strain. Among the tested analogs, four compounds (A-06, A-11, A-12, and A-15) exhibited significant anti-leishmanial activity with EC50 value ranges from 8.9 to 21.96 µM against amastigote forms of tested L. infantum strain with SI ranges of 1.0 to 4.3. From the activity results it was found that A-11 was the most active compound in both promastigote and amastigotes forms with EC50 values 8.53 and 8.90 µM respectively. In-silico ADME prediction studies depicted that the titled compounds obeyed Lipinski's rule of five as that of the approved marketed drugs. The predicted in-silico toxicity profile also confirmed that the tested compounds were non-toxic. Finally, molecular docking and molecular dynamics study was also performed for significantly active compound (A-11) in order to study it's putative binding pattern at the active site of the selected leishmanial trypanothione reductase target as well as to understand the stability pattern of target-ligand complex for 100 ns. Single crystal XRD of compound A-08 revealed that the compound crystallizes in monoclinic C2/c space group and showed interesting packing arrangements.

The Convalescent Plasma Craze! Where Does India Stand?

India becomes the country with second highest number of coronavirus disease 2019 (COVID-19) cases (59,03,932) as of September 2020. As the world debates various treatment options, the current pandemic has led to the resurgence of an ancient technique, namely convalescent plasma therapy. Although it has been in use from the late 19th century, it is an uncharted territory for most developing nations. In this article, we have discussed the pros and cons of convalescent plasma transfusion in COVID-19 patients. Articles discussed in this review have been obtained from search engines, namely PubMed, Scopus, and Embase. We have also expressed our viewpoint on the feasibility and logistical challenges of convalescent plasma use in India.

1,2,3,4-Tetrahydroisoquinoline (THIQ) as privileged scaffold for anticancer de novo drug design.

Introduction: Cancer is a dreadful disorder that is emerging as one of the leading causes of mortality across the globe. The complex tumor environment, supplemented with drawbacks of the existing drugs, has made it a global health concern. The Tetrahydroisoquinoline (THIQ) ring holds an important position in medicinal chemistry due to its wide range of pharmacological properties. Several THIQ based natural products have been previously explored for their antitumor properties, making it a vital scaffold for anticancer drug design.Areas covered: This review article addresses the potential of THIQ as anticancer agents. Various medicinal chemistry strategies employed for the design and development of THIQ analogs as inhibitors or modulators of relevant anticancer targets have been discussed in detail. Moreover, the common strategies employed for the synthesis of the core scaffold are also highlighted.Expert opinion: Evidently, THIQs have tremendous potential in anticancer drug design. Some of these analogs exhibited potent activity against various cancer molecular targets. However, there are some drawbacks, such as selectivity that need addressing. The synthetic ease for constructing the core scaffold complimented with its reactivity makes it ideal for further structure-activity relationship studies. For these reasons, THIQ is a privileged scaffold for the design and development of novel anticancer agents.