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 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.

Novel derivatives of Nicotinic acid as Promising anticancer agents

2020 ◽  
Vol 20 ◽  
Author(s):  
Nisha Jain ◽  
Divya Utreja ◽  
Komalpreet Kaur ◽  
Palak Jain
Keyword(s):  
Nicotinic Acid ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Biological Properties ◽  
Superior Effect ◽  
Nicotinamide Derivatives ◽  
Considerable Work ◽  
Synthetic Approaches ◽  
Nitrogen Containing Compounds ◽  
Derivatives Of

Background: Cancer has become the second leading cause of death worldwide. Despite of the availability of significant number of anticancer agents, cancer is still incurable especially at the last stages. Remarkable targets for anticancer research and drug discovery are heterocyclic compounds and among them superior effect has been shown by the nitrogen containing compounds than non-nitrogen containing compounds. Nicotinic acid, a nitrogen containing moiety and its derivatives have gained an immense importance in the development of anticancer drugs owing to the wide variety of biological properties displayed by them. Objective: The objective of this review is to provide researchers the information about various synthetic approaches used for the synthesis of anticancer drugs of nicotinic acid from 2001 onwards and to reveal their application and importance in the treatment of this dreadful disease. Conclusion: As indicated by this review, considerable work has been done in terms of synthesis and investigation of anticancer potential of nicotinamide derivatives. The information provided in this article may be of great value for the researchers seeking to develop efficient anticancer drugs.

The progress of the anticancer agents related to the microtubules target

2020 ◽  
Vol 20 ◽  
Author(s):  
Olagoke Zacchaeus Olatunde ◽  
Jianping Yong ◽  
Canzhong Lu
Keyword(s):  
Side Effects ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Mitotic Spindle ◽  
Stabilizing Agents

: Anticancer drugs based on the microtubules target are potent mitotic spindle poison agents, which interacted directly with the microtubules, and were classified as microtubule-stabilizing agents and microtubule-destabilizing agents. Researchers have worked tremendously towards the improvements of anticancer drugs, in terms of improving the efficacy, solubility and reducing the side effects, which brought about advancement in chemotherapy. In this review, we focused on describing the discovery, structures and functions of the microtubules as well as the progress of anticancer agents related to the microtubules, which will provide adequate references for researchers.

Progress and development of C-3, C-6, and N-9 position substituted carbazole integrated molecular hybrid molecules as potential anticancer agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Pratibha Mehta Luthra ◽  
Nitin Kumar
Keyword(s):  
Biological Activity ◽  
Side Effects ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Structural Motif ◽  
Hybrid Compounds ◽  
Hybrid Molecules ◽  
Anticancer Mechanism ◽  
Pharmacologically Active

Abstract: The carbazole skeleton, a key structural motif occurring naturally or chemically synthesized, have shown various biological activities. Molecular hybridization based on the combination of two or more bioactive pharmacophores has been an important tool to convert the potent structural leads to form new hybrid compounds with improved biological activity. In recent years, modifications/substitutions of the carbazole motif at C3, C6, N9 position have been carried to develop novel carbazole based potential anticancer agents in the cancer therapy. In the last fifteen years, several compounds based on carbazole core integrated to pharmacologically active molecular hybrid having active pharmacophore such as 1,3,4-thiadiazole, thiazole, guanidine, sulfonamides, glyoxamides, imidazole, phenanthrene, rhodamine, chalcones, imidazopyridine, platinum 2H-chromen-2-one, hydrazones, piperazine, Isoxazole-thiadiazole, pyrazole etc. have been synthesized showing anticancer profile at sub-micromolar to nano-molar concentrations. We have thoroughly reviewed the design, progress and development of C-3, C-6, and N-9 position substituted carbazole derivatives integrated with various medicinally active pharmacophore as potential anticancer agents evaluated against various cancer cell lines. Additionally, the anticancer mechanism and in vivo activity of the reported compounds have been discussed. This study will support in designing of a new pharmacophore that can be linked to carbazole motif for development for new, potent and target specific anticancer drugs with improved pharmacokinetics and minimal side effects.

scholarly journals Monofunctional Platinum(II) Anticancer Agents

2021 ◽  
Vol 14 (2) ◽  
pp. 133
Author(s):  
Suxing Jin ◽  
Yan Guo ◽  
Zijian Guo ◽  
Xiaoyong Wang
Keyword(s):  
Drug Resistance ◽  
Side Effects ◽  
Cancer Cells ◽  
General Formula ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Platinum Drugs ◽  
Cellular Distribution ◽  
Platinum Anticancer Drugs ◽  
Tumor Selectivity

Platinum-based anticancer drugs represented by cisplatin play important roles in the treatment of various solid tumors. However, their applications are largely compromised by drug resistance and side effects. Much effort has been made to circumvent the drug resistance and general toxicity of these drugs. Among multifarious designs, monofunctional platinum(II) complexes with a general formula of [Pt(3A)Cl]+ (A: Ammonia or amine) stand out as a class of “non-traditional” anticancer agents hopeful to overcome the defects of current platinum drugs. This review aims to summarize the development of monofunctional platinum(II) complexes in recent years. They are classified into four categories: fluorescent complexes, photoactive complexes, targeted complexes, and miscellaneous complexes. The intention behind the designs is either to visualize the cellular distribution, or to reduce the side effects, or to improve the tumor selectivity, or inhibit the cancer cells through non-DNA targets. The information provided by this review may inspire researchers to conceive more innovative complexes with potent efficacy to shake off the drawbacks of platinum anticancer drugs.

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 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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