Carbazole Scaffold in Medicinal Chemistry and Natural Products: A Review from 2010-2015

Abstract

9H-carbazole is an aromatic molecule that is tricyclic in nature, with two benzene rings fused onto a 5-membered pyrrole ring. Obtained from natural sources or by synthetic routes, this scaffold has gained much interest due to its wide range of biological activity upon modifications, including antibacterial, antimalarial, anticancer, and anti-Alzheimer properties. This review reports a survey of the literature on carbazole-containing molecules and their medicinal activities from 2010 through 2015. In particular, we focus on their in vitro and in vivo activities and summarize structure-activity relationships (SAR), mechanisms of action, and/or cytotoxicity/selectivity findings when available to provide future guidance for the development of clinically useful agents from this template.

Anticancer Activity of Mukonal Against Human Laryngeal Cancer Cells Involves Apoptosis, Cell Cycle Arrest, and Inhibition of PI3K/AKT and MEK/ERK Signalling Pathways

“…Moreover, total synthesis of Mukonal has also been reported previously [ 8 ]. Mukonal has been reported to exhibit antimicrobial and antioxidant activities [ 9 ]. However, the anticancer activity of Mukonal has not been thoroughly examined and the antiproliferative effects of Mukonal have not been evaluated against AMC-HN-8 laryngeal cancer cells.…”

More Than Resveratrol: New Insights into Stilbene-Based Compounds

“…Based on the statement that a chemical scaffold is defined as the structural core of a chemical compound [1], the concept of scaffold is a starting point in the design and development of new frameworks and gives a new lease of life to well-known structures. There is abundant literature [1][2][3][4][5][6][7][8][9][10][11][12] that presents various chemical frames and highlights the importance of this concept in different disciplines linked with drug discovery such as chemistry, pharmacy, and medicine. Considering a wide range of biological activities and a plethora of possible modifications, the stilbene is one of the most potent scaffolds in medicinal chemistry [2,13,14].…”

Synthesis and In Vitro Antitumor Evaluation of Some Carbazole‐Based Thiazole, Thiophene, and 1,3,4‐Thiadiazole Derivatives

“…Carbazoles and their related analogues are of particular interest in the areas of synthetic organic chemistry and pharmaceutical applications owing to their planar tricyclic frame and pervasive biological activities. [1][2][3][4] Carbazoles exist in many bioactive natural molecules [5] and display diverse bioactivities including antioxidant, [6] antimicrobial, [7] anticancer, [8] neuroprotective, [9] anti-inflammatory, [10] antihistamic, [11] antiviral, [12] anticonvulsant, [13] and anti-HIV functions. [14] The carbazole derivative, Celiptium (Figure 1), is a known drug used for the treatment of metastatic breast cancer.…”