Papers by Mr. Rajat Goyal
Sustainable Chemistry and Pharmacy, Oct 1, 2021
Abstract The exhaustive exploration of the conventional synthetic approaches for the synthesis of... more Abstract The exhaustive exploration of the conventional synthetic approaches for the synthesis of nitrogen and sulphur containing heterocyclic moieties has diverted the attention of researchers towards novel eco-friendly strategies of these compounds. Several green chemistry-based synthetic methods like multi-component single pot reaction, recyclable green-based catalyst, green solvent, reusable solvent, ultrasound-mediated synthesis, the solvent-free and microwave-assisted technique have been developed for the synthesis of thiazole derivatives with anticancer potential. According to the cancer society, almost 14.1 million cancer cases and about 8.2 million deaths due to cancer have been reported, which implies that one of every seven deaths occurs due to cancer disease. The thiazole scaffold is contained in more than 18 FDA-approved drugs, as well as, in several experimental formulations. Among them, alpelisib, a thiazole-based drug with the brand name Pigray®, was approved in 2019 for the treatment of breast cancer. The goal of the present review is to highlight the recent advancements in the green chemistry-based synthesis of thiazole derivatives with the discussion of their structure-activity relationship. Based on innovative eco-friendly reports in synthetic literature, this paper compiled the green strategies-based development of thiazole derivatives from 2012 till now with effective anticancer potential.
Current Traditional Medicine
: Generally, Ayurvedic or herbal products are considered safe to use. According to a report, more... more : Generally, Ayurvedic or herbal products are considered safe to use. According to a report, more than 50% of the global population depends upon herbal products. To meet the global demand for ayurvedic products, more and more herbal plants are analyzed for their active constituents and health benefits. Moringa oleifera is one such plant that is analyzed for its therapeutic benefits. Various parts of this plant, such as the leaves, roots, seed, bark, fruit, flowers, and immature pods, act as cardiac and circulatory stimulants with antipyretic, antitumor, anti-inflammatory, antiepileptic, diuretic, antiulcer, antispasmodic, antihypertensive, cholesterol-lowering, antidiabetic, antioxidant, antibacterial, hepatoprotective, and antifungal activities. This review is about the chemical composition of this tree’s market preparation and its different applications
Current Traditional Medicine
: Nature always has enough spirit and resilience to transform our limited vision. Herbal medicine... more : Nature always has enough spirit and resilience to transform our limited vision. Herbal medicines include products prepared from natural herbs which are employed to treat several diseases. In India, about 80% of drugs are of herbal origin. Nowadays, people are much more aware of the various side effects of synthetic drugs, which have molded their interest in herbal products and herbal remedies. In history, various infectious diseases or pandemic conditions have been treated or controlled with herbal medicines. Many herbal plants like Emblica officinalis (Euphorbiaceae), Withania somnifera (Solanaceae), Swertia chirata (Gentianaceae), Asparagus racemosus (Liliaceae), and Vinca rosea/Catharanthus roseus (Apocynaceae) have been reported to be of high medicinal values and preferred in the development of many newer drugs. The active component from plant extract is isolated, standardized, and undergoes safety trials for validation. Novel drug development from herbs is the amalgamation of practices of native systems of medicine and quite a lot of therapeutic experience of earlier generations. It is also believed that most herbal contents are safe, cheap, and easily available. Herbal drugs are useful in various diseased and pathogenic conditions like tuberculosis, cancer, diabetes, AIDS, jaundice, skin diseases, etc. Many countries with ancient cultures like India, Egypt, and America still use various herbal-based medications. Research for future herbal product development is increasing worldwide. Therefore, taking into consideration future perceptions of herbal remedies, this review deals with the present status and future exploration in the development of herbal drugs as modern beneficial agents for treating various infectious diseases and related pharmacological problems.
Frontiers in Oncology
There are more than two hundred fifty different types of cancers, that are diagnosed around the w... more There are more than two hundred fifty different types of cancers, that are diagnosed around the world. Prostate cancer is one of the suspicious type of cancer spreading very fast around the world, it is reported that in 2018, 29430 patients died of prostate cancer in the United State of America (USA), and hence it is expected that one out of nine men diagnosed with this severe disease during their lives. Medical science has identified cancer at several stages and indicated genes mutations involved in the cancer cell progressions. Genetic implications have been studied extensively in cancer cell growth. So most efficacious drug for prostate cancer is highly required just like other severe diseases for men. So nutraceutical companies are playing major role to manage cancer disease by the recommendation of best natural products around the world, most of these natural products are isolated from plant and mushrooms because they contain several chemoprotective agents, which could reduce t...
Frontiers in Pharmacology
Endometrial cancer (EC) is the sixth most prevalent type of cancer among women. Kinases, enzymes ... more Endometrial cancer (EC) is the sixth most prevalent type of cancer among women. Kinases, enzymes mediating the transfer of adenosine triphosphate (ATP) in several signaling pathways, play a significant role in carcinogenesis and cancer cells’ survival and proliferation. Cyclin-dependent kinases (CDKs) are involved in EC pathogenesis; therefore, CDK inhibitors (CDKin) have a noteworthy therapeutic potential in this type of cancer, particularly in EC type 1. Natural compounds have been used for decades in the treatment of cancer serving as a source of anticancer bioactive molecules. Many phenolic and non-phenolic natural compounds covering flavonoids, stilbenoids, coumarins, biphenyl compounds, alkaloids, glycosides, terpenes, and terpenoids have shown moderate to high effectiveness against CDKin-mediated carcinogenic signaling pathways (PI3K, ERK1/2, Akt, ATM, mTOR, TP53). Pharmaceutical regimens based on two natural compounds, trabectedin and ixabepilone, have been investigated in h...
Asian Journal of Chemistry, 2022
Thiazolopyrimidine is a nitrogen and sulphur containing heterocyclic aromatic molecule. The bicyc... more Thiazolopyrimidine is a nitrogen and sulphur containing heterocyclic aromatic molecule. The bicyclic compound is made by fusing two aromatic rings, thiazole and pyrimidine and replacing one carbon atom with nitrogen and sulphur. The current present work covers a wide range of methods for synthesizing thiazolopyrimidine and its derivatives using a variety of catalysts, solvent medium and microwave irradiation with a goal of achieving a high yield and rapid separation of the product. This article describes the evolution of thiazolopyrimidine as antimicrobial, antiviral, anti-Parkinson, anticancer, anti-inflammatory as well as its structure-activity relationship and potential mode of action for future research. It also includes a list of current patents filed/granted linked to various pharmacological activities in the previous few years.
Materials Today Chemistry, 2020
Despite the adverse effects of microbial hazards on public health, major pharmaceutical firms hav... more Despite the adverse effects of microbial hazards on public health, major pharmaceutical firms have left the field of anti-infective development and a dramatic reduction in the number of researcher'sintricated in the quest for new specific anti-infective leads. In the non-existence of an efficient forum for antibiotics development and over usage in human beings and animals, bacteria have demoralized this potential by gradually establishing the resistance toward most of the antibiotics used. Thus, the production of novel and successful anti-infectivedrugs is urgently required to combat this resistance. Hydrazones and hydrazides have mounted as a key-skeleton for the development of active drugs, due to their important biological and pharmacological profiles.Hydrazones are being manufactured as medicines by various investigators to fight against the ailments with maximal effects and minimal toxicity.This paper focuses on the outline of the literature results of recent years, incorporating the work on the anti-infective profileof Manuscript File Click here to view linked References 2 hydrazoneanalogues. This review may also act as an excellent basisfor the development of new derivatives of hydrazone as potential anti-infective mediators.
Central Nervous System Agents in Medicinal Chemistry, 2022
Background: Malaria parasite strains are resistant to the therapeutic effect of prophylactics med... more Background: Malaria parasite strains are resistant to the therapeutic effect of prophylactics medicines presently available. This resistance now poses a significant challenge to researchers to beat malaria parasitic infections. Strategies such as investigating newer hybrid chemical entities and specified drug targets may help us spot new efficient derivatives that bind to the parasites in a more specific manner and inhibit their growth. Objective: To scientifically perform the experimental, pharmacological, and computational studies of pyrazole-based furanone hybrids as novel antimalarial agents. Methods: A series of new furanone-based pyrazole derivatives were synthesized and investigated as potential antimalarial agents by performing in vitro antimalarial activity. To get further optimization, these synthesized derivatives were virtually screened based on ADME-T filters, and molecular docking studies were also accomplished on the crystal structures of Plasmodium falciparum lactate...
Drug Repurposing for Emerging Infectious Diseases and Cancer, 2023
Journal of Experimental Biology and Agricultural Sciences
Sexuality has become a medical issue in the context of aging due to a variety of aspects, such as... more Sexuality has become a medical issue in the context of aging due to a variety of aspects, such as growing life expectancy, an optimistic societal paradigm that indorses sexuality as significant for the superiority of life with age, and the medicalization of sexuality with the emergence of remedial medicines to extravagance sexual dysfunction. At any age, a reduction in the desire for sexual activity or inadequate performance of sexual intercourse is considered atypical and requires a medicinal treatment response. However, despite concerns that this is leading to an unhealthy obsession with sexuality from a medical perspective, this line of thinking is likely to continue. In this context, people can identify and take advantage of sexual problems. Sexual desire and performance are affected by normal physiological changes associated with aging in both genders. Medical experts must understand these changes to optimize sexual functioning in older patients. Sexual health can only be impro...
Frontiers in Pharmacology
siRNA interference, commonly referred to as gene silence, is a biological mechanism that inhibits... more siRNA interference, commonly referred to as gene silence, is a biological mechanism that inhibits gene expression in disorders such as cancer. It may enhance the precision, efficacy, and stability of medicines, especially genetic therapies to some extent. However, obstacles such as the delivery of oligonucleotide drugs to inaccessible areas of the body and the prevalence of severe side effects must be overcome. To maximize their potential, it is thus essential to optimize their distribution to target locations and limit their toxicity to healthy cells. The action of siRNA may be harnessed to delete a similar segment of mRNA that encodes a protein that causes sickness. The absence of an efficient delivery mechanism that shields siRNA from nuclease degradation, delivers it to cancer cells and releases it into the cytoplasm of specific cancer cells without causing side effects is currently the greatest obstacle to the practical implementation of siRNA therapy. This article focuses on c...
Nanotechnology in Functional Foods
Critical Reviews in Food Science and Nutrition
Breast cancer (BC) is the most prevalent neoplasm among women. Genetic and environmental factors ... more Breast cancer (BC) is the most prevalent neoplasm among women. Genetic and environmental factors lead to BC development and on this basis, several preventive – screening and therapeutic interventions have been developed. Hormones, both in the form of endogenous hormonal signaling or hormonal contraceptives, play an important role in BC pathogenesis and progression. On top of these, breast microbiota includes both species with an immunomodulatory activity enhancing the host’s response against cancer cells and species producing proinflammatory cytokines associated with BC development. Identification of novel multitargeted therapeutic agents with poly-pharmacological potential is a dire need to combat advanced and metastatic BC. A growing body of research has emphasized the potential of natural compounds derived from medicinal plants and microbial species as complementary BC treatment regimens, including dietary supplements and probiotics. In particular, extracts from plants such as Artemisia monosperma Delile, Origanum dayi Post, Urtica membranacea Poir. ex Savigny, Krameria lappacea (Dombey) Burdet & B.B. Simpson and metabolites extracted from microbes such as Deinococcus radiodurans and Streptomycetes strains as well as probiotics like Bacillus coagulans and Lactobacillus brevis MK05 have exhibited antitumor effects in the form of antiproliferative and cytotoxic activity, increase in tumors’ chemosensitivity, antioxidant activity and modulation of BC – associated molecular pathways. Further, bioactive compounds like 3,3’-diindolylmethane, epigallocatechin gallate, genistein, rutin, resveratrol, lycopene, sulforaphane, silibinin, rosmarinic acid, and shikonin are of special interest for the researchers and clinicians because these natural agents have multimodal action and act via multiple ways in managing the BC and most of these agents are regularly available in our food and fruit diets. Evidence from clinical trials suggests that such products had major potential in enhancing the effectiveness of conventional antitumor agents and decreasing their side effects. We here provide a comprehensive review of the therapeutic effects and mechanistic underpinnings of medicinal plants and microbial metabolites in BC management. The future perspectives on the translation of these findings to the personalized treatment of BC are provided and discussed.
Frontiers in Cell and Developmental Biology, 2021
Prostate cancer is the most common type of cancer among men and the second most frequent cause of... more Prostate cancer is the most common type of cancer among men and the second most frequent cause of cancer-related mortality around the world. The progression of advanced prostate cancer to castration-resistant prostate cancer (CRPC) plays a major role in disease-associated morbidity and mortality, posing a significant therapeutic challenge. Resistance has been associated with the activation of androgen receptors via several mechanisms, including alternative dehydroepiandrosterone biosynthetic pathways, other androgen receptor activator molecules, oncogenes, and carcinogenic signaling pathways. Tumor microenvironment plays a critical role not only in the cancer progression but also in the drug resistance. Numerous natural products have shown major potential against particular or multiple resistance pathways as shown by in vitro and in vivo studies. However, their efficacy in clinical trials has been undermined by their unfavorable pharmacological properties (hydrophobic molecules, ins...
Frontiers in Pharmacology
Ovarian cancer, and particularly its most frequent type, epithelial ovarian carcinoma, constitute... more Ovarian cancer, and particularly its most frequent type, epithelial ovarian carcinoma, constitutes one of the most dangerous malignant tumors among females. Substantial evidence has described the potential of phytochemicals against ovarian cancer. The effect of natural compounds on endoplasmic reticulum (ER) stress is of great relevance in this regard. In ovarian cancer, the accumulation of misfolded proteins in the ER lumen results in decompensated ER stress. This leads to deregulation in the physiological processes for the posttranslational modification of proteins, jeopardizes cellular homeostasis, and increases apoptotic signaling. Several metabolites and metabolite extracts of phytochemical origin have been studied in the context of ER stress in ovarian cancer. Resveratrol, quercetin, curcumin, fucosterol, cleistopholine, fucoidan, and epicatechin gallate, among others, have shown inhibitory potential against ER stress. The chemical structure of each compound plays an important...
Insights on fluoroquinolones in cancer therapy: chemistry and recent developments, 2020
Cancer is a very risky life-threatening disease having most formidable afflictions in the world. ... more Cancer is a very risky life-threatening disease having most formidable afflictions in the world. Several anticancer agents are commercially accessible, however, the emergence of acquired drug resistance along with extreme adverse effects of these clinically used anticancer medications are major barriers to the effective chemotherapy. Thus, it is recommended to rationally design the newer drugs with few side effects. Fluoroquinolone derivatives are of pivotal interest for researchers due to their admirable pharmacological and pharmacokinetic profiles. They exhibit several favourable characteristics including, higher bioavailability, excellent tissue penetration and relatively low prevalence of adverse and toxic effects. Due to their potential interventions in carcinogenesis and mutagenesis, the focus of the area of research is nowadays shifting towards anticancer aspects of these compounds. This review shows the recent advancements in the development of novel fluoroquinolones as potential anticancer and cytotoxic agents and structure-activity relationships along with the possible modes of action for further development and recent patents filed/granted related to anticancer activity from the last few years have also been tabulated. Also, this review is an attempt to focus on the various upcoming aspects of fluo-roquinolones and provides a newer outlook on the possible roles of fluoroquinolones in the treatment of cancer. Scientific information identified in this paper is expected to be useful for aspiring researchers working on the anticancer activity of fluoroquinolones.
Uploads
Papers by Mr. Rajat Goyal