ARTICLE INFO ABSTRACTProtein kinases have important role in cell proliferation & differentiation of cell. They involved in diverse biological processes like growth, differentiation, metabolism and apoptosis in response to external and internal stimuli, mediator of signaling cascade. Tyrosine kinases are enzymes that selectively phosphorylates tyrosine residue in different substrates. Over expression of these tyrosine kinases receptor cause development of human cancer. So lot of work is done to understand role of tyrosine kinases in the pathophysiology of cancer. Defective regulation of growth processes plays a role in the genesis and progression of most type of cancer. Oncogenic activation of tyrosine kinase due to mutation, autocrine-paracrine stimulation in cancer cells can be blocked by selective tyrosine kinase inhibitors and thus considered as a promising approach for treatment of cancer. This review describes the role of growth factors in development of cancer & the role of TK inhibitors or growth blockers on treating cancer. This review article describes the mechanism of action, structures, and side effects of potent protein kinase inhibitors.
Background:
Cancer is a complex disease in which some of the cells grow uncontrollably and spread to other parts of the body.
Objective: The present study focuses on molecular docking and synthesis of novel flavone derivatives substituted with heterocyclic rings.
Objective:
The present study focuses on molecular docking and synthesis of novel flavone derivatives substituted with heterocyclic rings.
Methods:
The anticancer activity of novel flavones against human aromatase enzyme using human breast cancer cell line MCF-7 through MTT assay was demonstrated. The synthesized compounds for the determination of single or double-strand DNA damage through the single-cell electrophoresis/comet assay were evaluated.
Results:
In this study, we found that the derivative 3M with Morpholine ring showed the highest anticancer potency against the MCF-7 cell line compared to that of other flavone derivatives. Compound 3T showed less cytotoxicity against the MCF-7 cell line.
Conclusion:
Based on the findings, flavone scaffolds can be selected as a skeleton for the development of heterocyclic amine-containing flavones with the potential to develop as anticancer drugs.
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