Indole: A Privileged Heterocyclic Moiety in the Management of Cancer

2021 ◽  
Vol 25 ◽  
Author(s):  
Reyaz Hassan Mir ◽  
Roohi Mohi-ud-din ◽  
Taha Umair Wani ◽  
Mohammad Ovais Dar ◽  
Abdul Jaleel Shah ◽  
...  

: Heterocyclic are a class of compounds that are intricately entwined into life processes. Almost more than 90% of marketed drugs carry heterocycles. Synthetic chemistry, in turn, allocates a cornucopia of heterocycles. Among the heterocycles, indole, a bicyclic structure consisting of a six-membered benzene ring fused to a five-membered pyrrole ring with numerous pharmacophores that generate a library of various lead molecules. Due to its profound pharmacological profile, indole got wider attention around the globe to explore it fully in the interest of mankind. The current review covers recent advancements on indole in the design of various anti-cancer agents acting by targeting various enzymes or receptors, including (HDACs), sirtuins, PIM kinases, DNA topoisomerases, and σ receptors.

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Marjan Talebi ◽  
Mohsen Talebi ◽  
Tahereh Farkhondeh ◽  
Jesus Simal-Gandara ◽  
Dalia M. Kopustinskiene ◽  
...  

AbstractChrysin has been shown to exert several beneficial pharmacological activities. Chrysin has anti-cancer, anti-viral, anti-diabetic, neuroprotective, cardioprotective, hepatoprotective, and renoprotective as well as gastrointestinal, respiratory, reproductive, ocular, and skin protective effects through modulating signaling pathway involved in apoptosis, oxidative stress, and inflammation. In the current review, we discussed the emerging cellular and molecular mechanisms underlying therapeutic indications of chrysin in various cancers. Online databases comprising Scopus, PubMed, Embase, ProQuest, Science Direct, Web of Science, and the search engine Google Scholar were searched for available and eligible research articles. The search was conducted by using MeSH terms and keywords in title, abstract, and keywords. In conclusion, experimental studies indicated that chrysin could ameliorate cancers of the breast, gastrointestinal tract, liver and hepatocytes, bladder, male and female reproductive systems, choroid, respiratory tract, thyroid, skin, eye, brain, blood cells, leukemia, osteoblast, and lymph. However, more studies are needed to enhance the bioavailability of chrysin and evaluate this agent in clinical trial studies. Graphic abstract


2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Khuram Shahzad Ahmad ◽  
Muntaha Talat ◽  
Shaan Bibi Jaffri ◽  
Neelofer Shaheen

AbstractConventional treatment modes like chemotherapy, thermal and radiations aimed at cancerous cells eradication are marked by destruction pointing the employment of nanomaterials as sustainable and auspicious materials for saving human lives. Cancer has been deemed as the second leading cause of death on a global scale. Nanomaterials employment in cancer treatment is based on the utilization of their inherent physicochemical characteristics in addition to their modification for using as nano-carriers and nano-vehicles eluted with anti-cancer drugs. Current work has reviewed the significant role of different types of nanomaterials in cancer therapeutics and diagnostics in a systematic way. Compilation of review has been done by analyzing voluminous investigations employing ERIC, MEDLINE, NHS Evidence and Web of Science databases. Search engines used were Google scholar, Jstore and PubMed. Current review is suggestive of the remarkable performance of nanomaterials making them candidates for cancer treatment for substitution of destructive treatment modes through investigation of their physicochemical characteristics, utilization outputs and long term impacts in patients.


2021 ◽  
Vol 17 ◽  
Author(s):  
Nidhi Kala ◽  
Kalpana Praveen Rahate

: Triazole is the main five-membered Nitrogen-containing basic heterocyclic ring system reported for their biological activities and compounds with multiple pharmacophores, which fetch together acquaintance of a target with sympathetic types of the molecule that might interact with the target. In addition, healthy, adaptable, and scalable chemistry must be employed to achieve the task. This characteristic feature of triazole would make a good template for a lead cohort library. The current review article focuses on recent advancements in triazole moiety as an anti-cancer agent with their mechanism pathways of synthesized analogues.


2021 ◽  
Vol 22 (18) ◽  
pp. 9861
Author(s):  
Boriss Strumfs ◽  
Romans Uljanovs ◽  
Kirils Velikijs ◽  
Peteris Trapencieris ◽  
Ilze Strumfa

Aziridination reactions represent a powerful tool in aziridine synthesis. Significant progress has been achieved in this field in the last decades, whereas highly functionalized aziridines including 3-arylated aziridine-2-carbonyl compounds play an important role in both medical and synthetic chemistry. For the reasons listed, in the current review we have focused on the ways to obtain 3-arylated aziridines and on the recent advances (mainly since the year 2000) in the methodology of the synthesis of these compounds via aziridination.


2015 ◽  
Author(s):  
Caroline Mignard ◽  
Olivier Duchamp ◽  
Fariba Nemati ◽  
Nathalie Cassoux ◽  
Sergio Roman-Roman ◽  
...  

Author(s):  
S. Baokar ◽  
K. Mane ◽  
A. Bhujbal ◽  
S. Pharande ◽  
G. Patil ◽  
...  

Worldwide the R & D divisions of Pharma industry are actively involved in the development of new therapeutic agents. These agents may be either new entities or partial structural modification of the existing one. The recent FDA statistics represent that the average number of drug filings are increasing every year in the thrust areas like anti-cancer agents, anti-diabetic, antibiotics, cardio-vascular drugs, respiratory drugs etc. Sodium glucose co-transporter-2(SGLT-2) inhibitors, dipeptidyl peptidase-4 (DPP-4) inhibitors and biguanides are effective oral anti-diabetic agents used in treatment of type 2 Diabetes Mellitus. Therefore, the necessity to explore and compare the existing analytical and bioanalytical assays used for determination of such drugs either single or in combination is crucial. Many methods were reported in the literature for the bio-analysis and analysis of four novel gliptins combinations, empagliflozin-linagliptin, empagliflozin-metformin HCl, linagliptin-metformin HCl, empagliflozin-linagliptin-metformin HCl combination with application on Glyxambi®, Synjardy®, Jentadueto®, Trijardy® XR tablets respectively. Furthermore, this review offered an overview of different methods used for determination of every drug alone as empagliflozin from SGLT-2 inhibitors, linagliptin from DPP-4 inhibitors and metformin from biguanides in a tabulated comparative way. Moreover, the current review emphasizes the most common stability indicating assays to be of interest to the analysts in the area of drug control. This review helps in understanding the further need for the development of analytical methods for the estimation of such drugs.


Author(s):  
NIKHIL ARUN CHAUDHARI ◽  
NINAD SATHE

Jeeraka, commonly known as cumin (Cuminum cyminum Linn.) (Family: Umbelliferae), is a popular herbal plant in traditional ayurvedic medicine, which has since long used as antioxidant, gastric stimulant, anti-flatulence, anti-diarrheal, sprue, anthelmintic, galactagogue, diuretic, astringent, carminative. This plant is pharmacologically and clinically evaluated for various activities like antioxidant, aphrodisiac, antimicrobial, hepato-protective, and anti-inflammatory. It is promulgated to possess a wide range of many phytochemical constituents. The current review is presented to give a comprehensive account of all anti-cancer activities of cumin. It will be helpful to create interest towards cumin and may be useful in developing new and economical anti-cancer formulations with more therapeutic value. The part used of the selected plant is seed. As per retrospective review cumin seed, its essential oil, ethanoic extract and 1­(2­Ethyl, 6­Heptyl) Phenol (EHP), a biologically active compound formerly extracted by benzene are found having anti-cancer activity against 13 different cell lines of various origins and 6 animal models. Also, it can be used as chemopreventive ingredient in the herbal anti-cancer formulation. Total 8 research articles, peer viewed research papers, abstracts and classical texts were reviewed.


2017 ◽  
Vol 9 (2) ◽  
pp. 860-865 ◽  
Author(s):  
Shubhransu Nayak ◽  
Archana Mukherjee ◽  
Soma Samanta

Endophytic microorganisms which include both bacteria and fungi colonise almost every plant species. In order to colonize the plant and compete with other microorganisms, they produce a plethora of secondary metabolites, including toxins, enzymes, antibiotics, anti-cancer, anti-inflammatory and antifungal compounds. Endophytic fungi can have profound impacts on plant communities which include abiotic and biotic stress tolerance, increase of biomass, decrease of water consumption and alteration of resource allocation, nitrogen fixation, increased drought resistance, thermal protection, survival under osmotic stress and degradation of pollutants. Though tuber crops are the second most important group of crop plants providing food energy to humans after cereals, less attention has been paid to the these traditional crops in general. Investigations regarding the association of endophytes with the tuber crops have been sparsely studied though in some tuber crops like cassava, sweet potato and yams, presence of endophytes have been reported. Hence from the scarcely available literature, in the current review an attempt was made to put light on the various beneficial activities of endophytes on tuber crops. These reports glorified many symbiotically associated endophytes to have antagonistic properties against many plant pathogens like Rhizoctoniasolani, Pythiumaphanidermatumand Sclerotiumrolfsii. Species like Rahnellawas resilient to cold shock, UV irradiation and antibiotics. Many diazotropihic and non-diazotropihicendophytic bacteria were involved in nitrogen fixation. Actinomycetesendophytes were novel sources of industrially important thermostableamylolytic enzymes. However, inspite of all these profound beneficial effects endophytic associations are still to be studied in many tuber crops like taro, elephant foot yam, greater yam etc. So this review put forward the urge to carry out comprehensive research on these important microbes on such important crops.


2020 ◽  
Vol 18 (3) ◽  
pp. 500-513 ◽  
Author(s):  
Weiqiang Chen ◽  
Hui-Jing Li ◽  
Qin-Ying Li ◽  
Yan-Chao Wu

The alkenylation reaction of benzoyl pyrroles occurred regioselectively at the C2-position of the pyrrole ring, without touching the benzene ring.


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