Recent Advances in the Synthesis and Anticancer Activity of Some Molecules Other Than Nitrogen Containing Heterocyclic Moeities

Akhtar, Md. Jawaid; Yar, Mohammad Shahar; Khan, Ahsan Ahmed; Ali, Zulphikar; Haider, Rafi

doi:10.2174/1389557516666161031121639

Cited by 20 publications

(17 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The chemical structure characteristics may affect the anticancer activities of a compound, such as the kind and position of substituents and the linker-chain length [ 52 , 53 , 54 ]. Hence, structural modifications on the eight subtypes of cytotoxic diterpenoids will become a research topic.…”

Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

“…Cancer stem cells (CSCs) are characterized by self-renewal, marked proliferation, and multilineage differentiation [ 54 , 55 , 56 , 57 ]. They have been proved to be the vital factor of malignant tumor recurrence and metastasis [ 54 , 55 , 56 , 57 ]. The theory of CSCs offers a new target and orientation for tumor therapy.…”

Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

See 1 more Smart Citation

Anti-Cancer Activities of Diterpenoids Derived from Euphorbia fischeriana Steud

et al. 2018

View full text Add to dashboard Cite

Euphorbia fischeriana Steud is an essential oriental folk medicine used for healing cancer, edema and tuberculosis. Recently, its anticancer activitity has attracted more attention. A volume of research has indicated that diterpenoids are the major anticancer active constituents from this medicinal herb. In this review, we aimed to provide a summary of the promising anticancer diterpenoids from this plant; many diterpenoids mentioned in this article are newly discovered diterpenoids. According to the carbon skeleton and substituents, they can be classified into eight subtypes: ent-abietane, daphnane, tigliane, ingenane, ent-atisane, ent-rosane, ent-kaurane, and lathyrane. Futhermore, their key anticancer mechanisms and protein targets of these compounds will be discussed. These natural diterpenoids could provide a reservoir for drug discovery.

show abstract

Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

Anti-Cancer Activities of Diterpenoids Derived from Euphorbia fischeriana Steud

et al. 2018

View full text Add to dashboard Cite

show abstract

“…Hybridization was a common method of drug development and design [11]. It was based on combining two or more different biologically active moieties in a single molecule to obtain the corresponding conjugated hybrid molecules [12]. These hybrid molecules may exhibit better activities than their precursors [13].…”

Section: Introductionmentioning

confidence: 99%

Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents

et al. 2019

View full text Add to dashboard Cite

To develop new antibacterial agents, a series of novel triazole-containing pyrazole ester derivatives were designed and synthesized and their biological activities were evaluated as potential topoisomerase II inhibitors. Compound 4d exhibited the most potent antibacterial activity with Minimum inhibitory concentration (MIC) alues of 4 µg/mL, 2 µg/mL, 4 µg/mL, and 0.5 µg/mL against Staphylococcus aureus, Listeria monocytogenes, Escherichia coli, and Salmonella gallinarum, respectively. The in vivo enzyme inhibition assay 4d displayed the most potent topoisomerase II (IC50 = 13.5 µg/mL) and topoisomerase IV (IC50 = 24.2 µg/mL) inhibitory activity. Molecular docking was performed to position compound 4d into the topoisomerase II active site to determine the probable binding conformation. In summary, compound 4d may serve as potential topoisomerase II inhibitor.

show abstract

“…Over the years several structural modifications were described and numerous hybrids were generated. Thereby, novel fused heterocyclic molecules with enhanced biological activity were identified which are applicable for the treatment of different diseases including cancer (Akhtar et al ., 2017).…”

Section: Introductionmentioning

confidence: 99%

Novel Isoquinolinamine and Isoindoloquinazolinone Compounds Exhibit Antiproliferative Activity in Acute Lymphoblastic Leukemia Cells

Roolf

Saleweski

Stein

et al. 2019

Biomolecules & Therapeutics

View full text Add to dashboard Cite

Nitrogen-containing heterocycles such as quinoline, quinazolinones and indole are scaffolds of natural products and have broad biological effects. During the last years those structures have been intensively synthesized and modified to yield new synthetic molecules that can specifically inhibit the activity of dysregulated protein kinases in cancer cells. Herein, a series of newly synthesized isoquinolinamine (FX-1 to 8) and isoindoloquinazolinone (FX-9, FX-42, FX-43) compounds were evaluated in regards to their anti-leukemic potential on human B- and T-acute lymphoblastic leukemia (ALL) cells. Several biological effects were observed. B-ALL cells (SEM, RS4;11) were more sensitive against isoquinolinamine compounds than T-ALL cells (Jurkat, CEM). In SEM cells, metabolic activity decreased with 10 μM up to 26.7% (FX-3), 25.2% (FX-7) and 14.5% (FX-8). The 3-(p-Tolyl) isoquinolin-1-amine FX-9 was the most effective agent against B- and T-ALL cells with IC50 values ranging from 0.54 to 1.94 μM. None of the tested compounds displayed hemolysis on erythrocytes or cytotoxicity against healthy leukocytes. Anti-proliferative effect of FX-9 was associated with changes in cell morphology and apoptosis induction. Further, influence of FX-9 on PI3K/AKT, MAPK and JAK/STAT signaling was detected but was heterogeneous. Functional inhibition testing of 58 kinases revealed no specific inhibitory activity among cancer-related kinases. In conclusion, FX-9 displays significant antileukemic activity in B- and T-ALL cells and should be further evaluated in regards to the mechanisms of action. Further compounds of the current series might serve as templates for the design of new compounds and as basic structures for modification approaches.

show abstract

Recent Advances in the Synthesis and Anticancer Activity of Some Molecules Other Than Nitrogen Containing Heterocyclic Moeities

Abstract: The review focused on the recent development of these derivatives, design and anticancer properties, thus providing with the most profound knowledge for the development of targeted based anticancer drugs.

Cited by 20 publications

References 0 publications

Anti-Cancer Activities of Diterpenoids Derived from Euphorbia fischeriana Steud

Anti-Cancer Activities of Diterpenoids Derived from Euphorbia fischeriana Steud

Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents

Novel Isoquinolinamine and Isoindoloquinazolinone Compounds Exhibit Antiproliferative Activity in Acute Lymphoblastic Leukemia Cells

Contact Info

Product

Resources

About