Pyridine moiety: An insight into recent advances in treatment of cancer

2021 ◽  
Vol 21 ◽  
Author(s):  
Rakesh Sahu ◽  
Rakhi Mishra ◽  
Rajnish Kumar ◽  
Salahuddin ◽  
Chandana Majee ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Antitumor Agents ◽  
Pyridine Moiety ◽  
Structure Activity ◽  
Wide Range ◽  
Global Health Issue ◽  
Effective Drugs ◽  
Published Research ◽  
Insight Into

: The incidence of cancer is increasing worldwide, affecting a vast majority of the human population. As new different anticancer agents are being developed now, the requirement is to deal somehow with them and evaluate their safety. Among them, pyridine based drugs are contributing a lot, as it is one of the imperative pharmacophores occurring synthetically as well as naturally in heterocyclic compounds, and having a wide range of therapeutic applications in the area of drug discovery, thereby offering many chances for further improvement in antitumor agents via acting onto numerous receptors of extreme prominence. Many pyridine derivatives have been reported to inhibit enzymes, receptors and many other targets for controlling and curing the global health issue of cancer. Nowadays, in combination with other moieties, researchers are focusing on the development of pyridine-based new derivatives for cancer treatment. Therefore, this review sheds light on the recent therapeutic expansions of pyridine together with its molecular docking, structure-activity-relationship, availability in the market, and a summary of recently patented and published research works that shall jointly help the scientists to produce effective drugs with the desired pharmacological activity.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

Accurate prediction of 195Pt NMR chemical shifts for a series of Pt(ii) and Pt(iv) antitumor agents by a non-relativistic DFT computational protocol

2014 ◽  
Vol 43 (14) ◽  
pp. 5409-5426 ◽  
Author(s):  
Athanassios C. Tsipis ◽  
Ioannis N. Karapetsas
Keyword(s):  
Dft Calculations ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Chemical Shifts ◽  
Accurate Prediction ◽  
Nmr Chemical Shifts ◽  
Relativistic Dft ◽  
Square Planar ◽  
Wide Range ◽  
Computational Protocol

Exhaustive benchmark DFT calculations reveal that the non-relativistic GIAO-PBE0/SARC-ZORA(Pt)∪6-31+G(d)(E) computational protocol predicts accurate 195Pt NMR chemical shifts for a wide range of square planar Pt(ii) and octahedral Pt(iv) anticancer agents.

scholarly journals Diarylureas as Antitumor Agents

2021 ◽  
Vol 11 (1) ◽  
pp. 374
Author(s):  
Alessia Catalano ◽  
Domenico Iacopetta ◽  
Maria Stefania Sinicropi ◽  
Carlo Franchini
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Anticancer Agent ◽  
Kinase Inhibitors ◽  
Antitumor Agents ◽  
Serine Threonine Kinase ◽  
Threonine Kinase ◽  
The Past ◽  
To Come ◽  
Come Into The Market

The diarylurea is a scaffold of great importance in medicinal chemistry as it is present in numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti-inflammatory properties. Some diarylureas, serine-threonine kinase or tyrosine kinase inhibitors, were recently reported in literature. The first to come into the market as an anticancer agent was sorafenib, followed by some others. In this review, we survey progress over the past 10 years in the development of new diarylureas as anticancer agents.

SLS-catalyzed Multi-component One-pot Reactions for the Convenient Synthesis of Spiro[indoline-3,4’-pyrano [2,3-c]pyrazole] Derivatives

2020 ◽  
Vol 07 ◽  
Author(s):  
Archana Dhakar ◽  
Archana Rajput ◽  
Ghazala Khanum ◽  
Dau D. Agarwal
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Ethyl Cyanoacetate ◽  
Reaction Times ◽  
Thermal Conditions ◽  
Biological Properties ◽  
High Yield ◽  
Spectroscopic Techniques ◽  
One Pot ◽  
Wide Range

Background,Objective: : spiro[indoline-3,4′-pyrano[2,3-c]pyrazoles] derivatives are an important heterocyclic compounds. These compounds shows wide range of biological properties and exhibits varied pharmaceutical applications. Pyranopyrazoles, which are basically fused heterocyclic compounds and act as vasodilators, hypertensive, hypoglycaemic, and anticancer agents. Methods: An efficient and micelle-promoted surfactant catalyzed synthesis of spiro[indoline-3,4′-pyrano[2,3-c]pyrazoles] derivatives have been achieved via one-pot four-component reaction of hydrazine hydrate (phenyl hydrazine), ethyl acetoacetate, malononitrile (ethyl cyanoacetate) and isatin under thermal conditions (at 60°C) in water as a solvent. Results: Sodium lauryl sulphate (SLS) used has been found to be an efficient and green catalyst. The compounds reported during this work were obtained in excellent yield, in a short duration of time and ease of work up. They were purified by recrystalization from ethanol, and also the synthesized compounds were characterized by various spectroscopic techniques. Conclusion: The method offers several advantages such as safe, cost-effective and catalyst easily recovered and reused for a minimum of five cycles, that confirms its good stability. Short reaction times, high yield and usage of eco-friendly catalyst and solvent are the key features of this methodology.

Naturally Occurring O-heterocycles as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Satya Kumar Avula ◽  
Biswanath Das ◽  
Rene Csuk ◽  
Ahmed Al-Harrasi
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Therapeutic Agents ◽  
Review Article ◽  
Drug Discovery And Development ◽  
Lead Compounds ◽  
Naturally Occurring ◽  
Structure Activity ◽  
Recent Advancement ◽  
Deadly Disease

: Cancer is a leading cause of death worldwide. Proper efficient drugs are required to treat this deadly disease. Natural products have long been a vital source of anticancer agents and they have generated various “lead compounds” suitable for drug developments. With the recent advancement of chemical synthesis and bioevaluation techniques these lead compounds of natural origins have been utilized for production of useful anticancer drugs. Among the naturally occurring bioactive compounds various O-heterocycles have been evaluated as remarkable cancer therapeutic agents. These compounds generally possess unique structures and novel mechanism of action. In the present review article, some selected O-heterocycles as promoting anticancer agents have been discussed in brief. Various natural sources and chemistry as well as bioactivities of these compounds have been described. The development of improved analogues of these compounds through synthetic modifications and efficient bioevaluation along with proper studies on structure-activity relationship and mechanism of actions has been mentioned. The article has demonstrated the recent relevance of naturally occurring O-heterocyclic compounds in current anticancer drug discovery and development scenario.

Thiosemicarbazones as Potent Anticancer Agents and their Modes of Action

2020 ◽  
Vol 20 (8) ◽  
pp. 638-661 ◽  
Author(s):  
Bhushan Shakya ◽  
Paras Nath Yadav
Keyword(s):  
Anticancer Agents ◽  
Antitumor Agents ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Side Chain ◽  
Inactive Compound ◽  
Cancer Breast ◽  
Wide Range ◽  
Ring Nitrogen ◽  
Tumor Types

: Thiosemicarbazones (TSCs) are a class of Schiff bases usually obtained by the condensation of thiosemicarbazide with a suitable aldehyde or ketone. TSCs have been the focus of chemists and biologists due to their wide range of pharmacological effects. One of the promising areas in which these excellent metal chelators are being developed is their use against cancer. TSCs have a wide clinical antitumor spectrum with efficacy in various tumor types such as leukemia, pancreatic cancer, breast cancer, non-small cell lung cancer, cervical cancer, prostate cancer and bladder cancer. To obtain better activity, different series of TSCs have been developed by modifying the heteroaromatic system in their molecules. These compounds possessed significant antineoplastic activity when the carbonyl attachment of the side chain was located at a position α to the ring nitrogen atom, whereas attachment of the side chain β or γ to the heterocyclic N atom resulted in inactive antitumor agents. In addition, replacement of the heterocyclic ring N with C also resulted in a biologically inactive compound suggesting that a conjugated N,N,S-tridentate donor set is essential for the biological activities of thiosemicarbazones. Several possible mechanisms have been implemented for the anticancer activity of thiosemicarbazones.

A Review: Synthesis and Pharmacological Profile of [1, 5]-Benzothiazepine

2021 ◽  
Vol 18 ◽  
Author(s):  
Shaik Khasimbi ◽  
Faraat Ali ◽  
Kumari Neha ◽  
Sharad Wakode ◽  
Garima Chauhan
Keyword(s):  
Anticancer Agents ◽  
Channel Blocker ◽  
Drug Research ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Chemical Transformations ◽  
Lead Discovery ◽  
Structure Activity ◽  
Wide Range ◽  
Relationship Of

: The 1, 5-benzothiazepine derivatives are of particular interest for lead discovery since they have been found active against different families of targets.1,5-Benzothaizepines representatives of benzologs of 1,4-thiazepine and one of the three possible benzo-condensed derivatives, i.e. the 1,5-benzothiazepines are useful compounds in the drug research which has stimulated the invention of a wide range of synthetic methods for their preparation and chemical transformations. 1,5-Benzothiazepine and its derivatives exhibit diverse biological activities such as tranquilizer, antidepressant, antihypertensive, calcium channel blocker, antimicrobial, anticancer, antifungal, anthelmintic, anti-diabetic, amyloid imagining agents and anticancer agents. This review also discusses the structure-activity relationship of the most potent compounds. It can act as an important tool for medicinal chemists to develop newer compounds possessing 1, 5-benzothiazepines moiety that could be better agents in terms of efficacy and safety.

Prospective Plant Based Anticancer Lead Molecules

2019 ◽  
Vol 18 (30) ◽  
pp. 2567-2583
Author(s):  
Prabhjot Kaur ◽  
Vikas Sharma
Keyword(s):  
Natural Products ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Present Review ◽  
Cross Resistance ◽  
Structure Activity ◽  
Key Points ◽  
Wide Range ◽  
Cause Of Deaths ◽  
Important Structure

Nature has been a source of a wide range of products being utilized for the treatment of various diseases like malaria, cancer, diabetes etc. Among these, cancer is emerging as a leading cause of deaths worldwide and the development of cross-resistance to already established drugs increases the need for novel anticancer drugs. To discover novel anticancer molecules, it is a necessity to unearth the molecules which can act as anticancer agents. Taking natural products in vision, phytoconstituents like terpenoids, flavones, glycosides and alkaloids might act as a major source of lead molecules. Considering the anticancer prospectives of phytoconstituents, different unknown lead molecules are summarized in this review. The present review highlights the representative studies of plant-based anticancer agents which are classified as per their phytochemical nature. Furthermore, important key points along with important structure-activity relationships points regarding selected lead molecules are also discussed.

scholarly journals Platinum and Palladium Polyamine Complexes as Anticancer Agents: The Structural Factor

2013 ◽  
Vol 2013 ◽  
pp. 1-29 ◽  
Author(s):  
M. P. M. Marques
Keyword(s):  
Anticancer Agents ◽  
Antitumor Agents ◽  
Structural Characteristics ◽  
Long Distance ◽  
Bridging Ligands ◽  
Structure Activity ◽  
Structural Preferences ◽  
Close Relationship ◽  
Interstrand Cross Links ◽  
Cross Links

Since the introduction of cisplatin to oncology in 1978, Pt(II) and Pd(II) compounds have been intensively studied with a view to develop the improved anticancer agents. Polynuclear polyamine complexes, in particular, have attracted special attention, since they were found to yield DNA adducts not available to conventional drugs (through long-distance intra- and interstrand cross-links) and to often circumvent acquired cisplatin resistance. Moreover, the cytotoxic potency of these polyamine-bridged chelates is strictly regulated by their structural characteristics, which renders this series of compounds worth investigating and their synthesis being carefully tailored in order to develop third-generation drugs coupling an increased spectrum of activity to a lower toxicity. The present paper addresses the latest developments in the design of novel antitumor agents based on platinum and palladium, particularly polynuclear chelates with variable length aliphatic polyamines as bridging ligands, highlighting the close relationship between their structural preferences and cytotoxic ability. In particular, studies by vibrational spectroscopy techniques are emphasised, allowing to elucidate the structure-activity relationships (SARs) ruling anticancer activity.

scholarly journals Synthesis and insight into the structure–activity relationships of 2-phenylbenzimidazoles as prospective anticancer agents

RSC Advances ◽  
2020 ◽  
Vol 10 (35) ◽  
pp. 20543-20551 ◽  
Author(s):  
Thi-Kim-Chi Huynh ◽  
Thi-Hong-An Nguyen ◽  
Thi-Cam-Thu Nguyen ◽  
Thi-Kim-Dung Hoang
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Lines ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Insight Into

Three series of 2-phenylbenzimidazoles obtained under simple and convenient pathways, were used to elucidate their SARs against three cancer cell lines: A549, MDA-MB-231 and PC3.

Sign in / Sign up

Export Citation Format

Share Document