scholarly journals Chirality in Anticancer Agents

2021 ◽  
Author(s):  
Jindra Valentová ◽  
Lucia Lintnerová
Keyword(s):  
Biological Activity ◽  
Antitumor Activity ◽  
Nucleic Acids ◽  
Anticancer Activity ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Biological Molecules ◽  
Therapeutic Activity ◽  
Specific Recognition

Many drugs are chiral and their therapeutic activity depends on specific recognition of chiral biomolecules. The biological activity of enantiomers can also differ drastically in terms of toxicity and pharmacokinetics. Chiral natural biological molecules, such as nucleic acids, enzymes are targeted molecules for the development of anticancer drugs. The interest in chiral agents is logically a result of the different interaction with biomolecules leading in the end consequence to improve anticancer activity and maybe to less undesirable effects. This review outlines the effects of chirality on the efficiency of anticancer metal-based agents and potential organic drugs. A variety of up-to-date examples of structurally diverse chiral agents exhibiting different mechanisms in their antitumor activity is presented.

Recent Design and Structure-Activity Relationship Studies on Modifications of DHFR Inhibitors as Anticancer Agents

2019 ◽  
Vol 26 ◽  
Author(s):  
Agnieszka Wróbel ◽  
Danuta Drozdowska
Keyword(s):  
Anticancer Activity ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Physicochemical Characterization ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Biological Research ◽  
Structure Activity ◽  
Dhfr Inhibitors

Background: Dihydrofolate reductase (DHFR) has been known for decades as a molecular target for antibacterial, antifungal and anti-malarial treatments. This enzyme is becoming increasingly important in the design of new anticancer drugs, which is confirmed by numerous studies including modelling, synthesis and in vitro biological research. This review aims to present and discuss some remarkable recent advances on the research of new DHFR inhibitors with potential anticancer activity. Methods: The scientific literature of the last decade on the different types of DHFR inhibitors has been searched. The studies on design, synthesis and investigation structure-activity relationship were summarized and divided into several subsections depending on the leading molecule and its structural modification. Various methods of synthesis, potential anticancer activity and possible practical applications as DHFR inhibitors of new chemical compounds were described and discussed. <p> Results: This review presents the current state of knowledge on the modification of known DHFR inhibitors and the structures and searching for over eighty new molecules, designed as potential anticancer drugs. In addition, DHFR inhibitors acting on thymidylate synthase (TS), carbon anhydrase (CA) and even DNA-binding are presented in this paper. <p> Conclusion: Thorough physicochemical characterization and biological investigations it is possible to understand structure-activity relationship of DHFR inhibitors. This will enable even better design and synthesis of active compounds, which would have the expected mechanism of action and the desired activity.

scholarly journals Ferrocene-Based Compounds with Antimalaria/Anticancer Activity

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3604 ◽  
Author(s):  
Sijongesonke Peter ◽  
Blessing Atim Aderibigbe
Keyword(s):  
Biological Activity ◽  
Anticancer Activity ◽  
Chronic Diseases ◽  
Anticancer Drugs ◽  
Drug Toxicity ◽  
Antimalarial Activity ◽  
Antimalarial Agents ◽  
Ferrocene Compounds

Malaria and cancer are chronic diseases. The challenge with drugs available for the treatment of these diseases is drug toxicity and resistance. Ferrocene is a potent organometallic which have been hybridized with other compounds resulting in compounds with enhanced biological activity such as antimalarial and anticancer. Drugs such as ferroquine were developed from ferrocene and chloroquine. It was tested in the 1990s as an antimalarial and is still an effective antimalarial. Many researchers have reported ferrocene compounds as potent compounds useful as anticancer and antimalarial agents when hybridized with other pharmaceutical scaffolds. This review will be focused on compounds with ferrocene moieties that exhibit either an anticancer or antimalarial activity.

Bestowal of Quinazoline Scaffold in Anticancer Drug Discovery

2020 ◽  
Vol 20 ◽  
Author(s):  
Rina Das ◽  
Dinesh K. Mehta ◽  
Meenakshi Dhanawat
Keyword(s):  
Dna Repair ◽  
Anticancer Activity ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Chemotherapeutic Agents ◽  
Special Focus ◽  
Significant Activity ◽  
Repair Enzyme ◽  
Treatment Regimens ◽  
Quinazoline Derivatives

Background: Cancer is one of the major causes of worldwide human mortality. A number of existing antineoplastic medications and treatment regimens are already working in the field and several new compounds are in different phases of clinical trials. An extensive series of anticancer drugs exists in the market, and studies suggest that these molecules are associated with different types of adverse side effects. Reduction of the cytotoxicity of drugs to the normal cells is a major problem in anticancer therapy. Therefore, researchers around the globe are involved in the development of more efficient and safer anticancer drugs. The output of extensive research is that the quinazoline scaffold and its various derivatives can be explored further as a novel class of cancer chemotherapeutic agents that has already shown promising activities against different tumours. Quinazoline derivatives have already occupied a crucial place in modern medicinal chemistry.Various research has been performed on quinazoline and their derivatives for anticancer activity and pharmacological importance of this scaffold has been well established. Objective: The aim of this review is to compile and highlight the developments concerning the anticancer activity of quinazoline derivatives as well as to suggest some new aspects on the expansion of anticancer activity of novel quinazoline derivatives as anticancer agents in the near future. Methods: Recent literature related to quinazoline derivatives endowed with encouraging anticancer potential is reviewed. With special focus on quinazoline moiety, this review offers a detailed account of multiple mechanisms of action of various quinazoline derivatives: inhibition of the DNA repair enzyme system, inhibition of EGFR, thymidylate enzyme inhibition and inhibitory effects for tubulin polymerization by which these derivatives have shown promising anticancer potential. Results: Exhaustive literature survey indicated that quinazoline derivatives are associated with properties of inhibiting EGFR and thymidylate enzyme. It was also found to be involved in disturbing tubulin assembly. Furthermore, quinazoline derivatives have been found to inhibit critical targets such as DNA repair enzyme. These derivatives have shown significant activity against cancer. Conclusion: In cancer therapy, Quinazoline derivatives seems to be quite promising and act through various mechanisms that are well established. This review has shown that quinazoline derivatives can further be explored for the betterment of chemotherapy. A lot of potential is still hidden which demands to be discovered for upgrading quinazoline derivatives efficacy.

1-[(2E)-3-Phenylprop-2-enoyl]-1H-benzimidazoles as anticancer agents: synthesis, crystal structure analysis and binding studies of the most potent anticancer molecule with serum albumin

MedChemComm ◽  
2015 ◽  
Vol 6 (11) ◽  
pp. 1942-1953 ◽  
Author(s):  
Veerendra Kumar A. Kalalbandi ◽  
J. Seetharamappa
Keyword(s):  
Crystal Structure ◽  
Antitumor Activity ◽  
Serum Albumin ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Spectral Methods ◽  
Crystal Structure Analysis ◽  
Selectivity Ratio ◽  
Binding Studies ◽  
Mechanism Of Interaction

The anticancer activity of 1H-benzimidazoles was studied against NCI 60 cell panel. Compound 3f showed antitumor activity with good to moderate selectivity ratio. Mechanism of interaction of 3f with protein was studied by spectral methods.

scholarly journals In the Search for New Anticancer Drugs, IV+ Antitumor Activity of Seleno-TEPA

1983 ◽  
Vol 38 (9) ◽  
pp. 1138-1141 ◽  
Author(s):  
Maria Konieczny ◽  
Peter L. Gutierrez ◽  
George Sosnovsky
Keyword(s):  
Antitumor Activity ◽  
Anticancer Activity ◽  
Anticancer Drugs ◽  
Human Cell ◽  
Human Cell Lines ◽  
Colony Assay ◽  
Selenium Analog ◽  
New Anticancer Drugs ◽  
Cell Colony

Abstract In order to test the effect of selenium on the anticancer activity of alkylating drugs, Seleno-TEPA (4), the selenium analog of the clinically used Thio-TEPA (1) was tested in vivo against the lymphocytic P 388 and lymphoid L1210 murine leukemias. Compound 4 is more active against P 388 leukemia than against L1210, and appears to be active over a narrower concentration range than Thio-TEPA (1). Compound 4 is less active against P 388 leukemia than 1, as evidenced by the T/C values of 164 for 4 and 239 for 1 at a dose of 4.2 mg/kg. The activity of 4 was also evaluated on the HL60 and K 562 human cell lines. Under the conditions of the cell colony assay technique, Seleno-TEPA (4) is less effective than Thio-TEPA (1).

scholarly journals Development of a Streptomyces venezuelae-Based Combinatorial Biosynthetic System for the Production of Glycosylated Derivatives of Doxorubicin and Its Biosynthetic Intermediates

2011 ◽  
Vol 77 (14) ◽  
pp. 4912-4923 ◽  
Author(s):  
Ah Reum Han ◽  
Je Won Park ◽  
Mi Kyeong Lee ◽  
Yeon Hee Ban ◽  
Young Ji Yoo ◽  
...  
Keyword(s):  
Biological Activity ◽  
Side Effects ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Important Determinant ◽  
Biosynthetic Enzymes ◽  
Streptomyces Venezuelae ◽  
Content Type ◽  
Biological Tool ◽  
Derivatives Of

ABSTRACTDoxorubicin, one of the most widely used anticancer drugs, is composed of a tetracyclic polyketide aglycone andl-daunosamine as a deoxysugar moiety, which acts as an important determinant of its biological activity. This is exemplified by the fewer side effects of semisynthetic epirubicin (4′-epi-doxorubicin). An efficient combinatorial biosynthetic system that can convert the exogenous aglycone ε-rhodomycinone into diverse glycosylated derivatives of doxorubicin or its biosynthetic intermediates, rhodomycin D and daunorubicin, was developed through the use ofStreptomyces venezuelaemutants carrying plasmids that direct the biosynthesis of different nucleotide deoxysugars and their transfer onto aglycone, as well as the postglycosylation modifications. This system improved epirubicin production from ε-rhodomycinone by selecting a substrate flexible glycosyltransferase, AknS, which was able to transfer the unnatural sugar donors and a TDP-4-ketohexose reductase, AvrE, which efficiently supported the biosynthesis of TDP-4-epi-l-daunosamine. Furthermore, a range of doxorubicin analogs containing diverse deoxysugar moieties, seven of which are novel rhodomycin D derivatives, were generated. This provides new insights into the functions of deoxysugar biosynthetic enzymes and demonstrates the potential of theS. venezuelae-based combinatorial biosynthetic system as a simple biological tool for modifying structurally complex sugar moieties attached to anthracyclines as an alternative to chemical syntheses for improving anticancer agents.

scholarly journals Advances of Benzimidazole Derivatives as Anticancer Agents: Bench to Bedside

2022 ◽  
Author(s):  
Kashif Haider ◽  
Mohammad Shahar Yar
Keyword(s):  
Cancer Research ◽  
Biological Activity ◽  
Anticancer Drugs ◽  
Broad Spectrum ◽  
Anticancer Agents ◽  
Therapeutic Potential ◽  
Structural Features ◽  
Clinical Development ◽  
Benzimidazole Derivatives ◽  
Antimitotic Agent

Benzimidazole is one of the privileged nitrogen-containing scaffolds known for its versatile diversified role in insecticides, pesticides, dyes, pigments and pharmaceuticals. Due to its electron-rich environment, structural features and binding potency of various therapeutic targets, benzimidazole derivatives exhibit a broad spectrum of biological activity that majorly includes antimicrobial, antifungal, analgesics, anti-diabetic and anticancer agents. Several benzimidazole scaffolds bearing drugs are clinically approved; they are used for various indications. For example, Bilastine, Lerisetron, Maribavir and Nocodazole are the most widely used benzimidazole-based marketed drugs available as an antihistamine, antiviral and antimitotic agent, respectively. Another example is the recently approved anticancer drug Binimetinib and Selumetinib, which are indicated for BRAF mutated melanoma and plexiform neurofibromas. Not only this, many benzimidazole-based anticancer drugs are in late phases of clinical development. Due to the vast therapeutic potential of benzimidazole scaffold in cancer research, medicinal chemists have gained a lot of attraction to explore it more and develop novel, highly effective and target-specific benzimidazole-based potential anticancer drugs.

scholarly journals Biological Activity of Phenolic Compounds in Extra Virgin Olive Oils through Their Phenolic Profile and Their Combination with Anticancer Drugs Observed in Human Cervical Carcinoma and Colon Adenocarcinoma Cells

Antioxidants ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 453 ◽  
Author(s):  
Jelena Torić ◽  
Anamaria Brozovic ◽  
Mirela Baus Lončar ◽  
Cvijeta Jakobušić Brala ◽  
Ana Karković Marković ◽  
...  
Keyword(s):  
Biological Activity ◽  
Olive Oil ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Biological Effect ◽  
Dependent Manner ◽  
Phenolic Profile ◽  
Virgin Olive Oils ◽  
Olive Oils

The roles of phenolics from olive oils as effective anticancer agents have been documented in various in vitro studies of different cancer cells lines, but the relationship between the phenolic profile of olive oil and its biological activity needs more elucidation. In this study, we analysed phenolic profiles of extra virgin olive oils (EVOOs) from different autochthonous cultivars from Croatia (Oblica, Bjelica, Buža, Žižolera) and investigated the biological effect of EVOO phenolic extracts (EVOO-PEs) on human cervical (HeLa) and human colon (SW48) cancer cell lines alone and in combination with cisplatin (cDDP), carboplatin (CBP), 5-fluorouracil (5-FU) and irinotecan. The quantitative evaluation of olive oil polyphenols was performed by HPLC-DAD and spectrophotometric analysis. The biological effect of EVOO-PEs alone and in combination with anticancer drugs was measured by MTT assay. Analysed EVOO-PEs differ in phenolic profile and inhibited HeLa and SW48 cells in a dose-dependent manner. Further, it is shown that EVOO-PEs (Oblica-Sea, Buža and Žižolera), in combination with anticancer drugs, increase the metabolic activity of HeLa and SW48 cells and have a protective role. These data imply careful consummation of olive oil during chemotherapy of cancer patients.

scholarly journals Gold Derivatives Development as Prospective Anticancer Drugs for Breast Cancer Treatment

2021 ◽  
Vol 11 (5) ◽  
pp. 2089
Author(s):  
Ileana Ielo ◽  
Domenico Iacopetta ◽  
Carmela Saturnino ◽  
Pasquale Longo ◽  
Maurilio Galletta ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Antitumor Activity ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Morphological Changes ◽  
Gold Complexes ◽  
In Vitro Proliferation ◽  
Square Planar ◽  
Planar Geometries

Commonly used anticancer drugs are cisplatin and other platinum-based drugs. However, the use of these drugs in chemotherapy causes numerous side effects and the onset of frequent drug resistance phenomena. This review summarizes the most recent results on the gold derivatives used for their significant inhibitory effects on the in vitro proliferation of breast cancer cell models and for the consequences deriving from morphological changes in the same cells. In particular, the study discusses the antitumor activity of gold nanoparticles, gold (I) and (III) compounds, gold complexes and carbene-based gold complexes, compared with cisplatin. The results of screening studies of cytotoxicity and antitumor activity for the gold derivatives show that the death of cancer cells can occur intrinsically by apoptosis. Recent research has shown that gold (III) compounds with square planar geometries, such as that of cisplatin, can intercalate the DNA and provide novel anticancer agents. The gold derivatives described can make an important contribution to expanding the knowledge of medicinal bioorganometallic chemistry and broadening the range of anticancer agents available, offering improved characteristics, such as increased activity and/or selectivity, and paving the way for further discoveries and applications.

scholarly journals The Importance of 2-AminoThiazole Schiff Bases as Antimicrobial and Anticancer Agents

2020 ◽  
Vol 31 (3) ◽  
pp. 46
Author(s):  
Shayma L. Abdulhadi ◽  
Maadh Q. Abdulkadir ◽  
May M. Al-Mudhafar
Keyword(s):  
Biological Activity ◽  
Schiff Base ◽  
Metal Complexes ◽  
Anticancer Activity ◽  
Schiff Bases ◽  
Anticancer Agents ◽  
Pharmaceutical Chemistry ◽  
Schiff Base Derivatives ◽  
Derivatives Of ◽  
Diverse Biological Activity

The pharmacophore 2-aminothiazole has an interesting role in pharmaceutical chemistry as this led to the synthesis of many types of compounds with diverse biological activity. Schiff base derivatives at the same time contribute to drug evolution importantly. In this review, the Schiff base derivatives of 2-aminothiazole formed and some of their metal complexes are being focused on, and the antimicrobial and anticancer activity of them is being illustrated.

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