Indole Derivatives as Anticancer Agents for Breast Cancer Therapy: A Review

Abstract

Breast cancer (BC) is the second most common cause of cancer-related deaths in women throughout the world. Multiple drugs have been approved by US-FDA for breast related malignancies. Frequent emergence of resistances creates the severe need of newer moieties that are free from such problems. Drugs targeting breast cancer have been observed to be based on the multiple mechanisms of action, and various indole based anticancer agents have also been explored. Moreover, indoles have promising anti-cancer potential; there has been the emphasis on the synthesis of indole derivatives to overcome problems faced by existing therapeutic agents. Taking into consideration the above-mentioned facts we have analyzed in detail the possible role of indole based anticancer agents typically for breast related malignancies. This is the first exhaustive review that jointly covers various synthetic anticancer indole derivatives and related signaling pathways by which these derivatives have shown promising anti-breast cancer potential.

Current research on anti-breast cancer synthetic compounds

“…Moreover, indoles have promising anti-cancer potential; there has been the emphasis on the synthesis of indole derivatives to overcome problems faced by existing therapeutic agents. 76 A series of indeno[1,2-b]indole-9,10-dione derivatives were synthesized as human casein kinase II (CK2) inhibitors. Comparison the relative ability of each compound to inhibit CK2, compound 69 (IC 50 ¼ 25 Â 10 À3 mM) ( Table 5) has a distinct antiproliferative effect against MCF-7 BC cells and was about orders of magnitude more selective.…”

<p>New Isatin–Indole Conjugates: Synthesis, Characterization, and a Plausible Mechanism of Their in vitro Antiproliferative Activity</p>

“…16,17 It is considered to be a beneficial motif in drug-discovery programs because of its biodiversity, versatility, and anticancer activity. [18][19][20][21] Previous evidence suggests that myriad indole-based compounds exert anticancer activities through various mechanisms, [22][23][24][25][26][27] suggesting the possibility of using the indole scaffold in anticancer drugs. Notably, anticancer indole-based molecules target several pathways, such as those involving tubulin polymerization, DNA topoisomerase, histone deacetylase, proto-oncogenes, and serine/threonine (PIM) kinase.…”

Synthesis, Characterization, Solution Behavior and Theoretical Studies of Pd(II) Allyl Complexes with 2-Phenyl-3H-indoles as Ligands

“…Indole is one of the most important heterocycles for its presence in bioactive natural products, pharmaceuticals, and agrochemicals [1][2][3][4][5][6][7][8][9]. Indole derivatives are not only "privileged structures" in Medicinal Chemistry [1][2][3][4]6,[10][11][12], due to their biological activity, but also valuable reagents for the design and synthesis of compounds with interesting properties and applications in a variety of fields [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19]. The construction and functionalization of indoles have been studied since long ago; however, and as mentioned by Prof. M. Bandini some years ago "this field had a formidable boom across the new millennium when catalysis started revolutionizing the chemistry of indole" [7].…”

“…Selected bond lengths (in Å) and angles (in deg. ): Pd1-Cl1, 2.4815(11); Pd1-N1, 2.124(4); Pd1-C17, 2.189(6); Pd1-C18, 2.127(9); Pd1-C19, 2.072(6); C18-C17, 1.379(7); C19-C18, 1.375(7); Cl1-Pd1-N1; 94.23(10); C17-Pd1-N1, 101.43(19); C19-Pd1-Cl1, 99.15(19); C19-Pd1-C17, 65.2(2).The central carbon atom of the allyl group C18 [Figure S1, (a)] is located out of the coordination plane of the palladium and on the same side as the C1 atom of the indole unit (endo-), therefore crystals of 2a contain the endoisomer (Figure 2, type A). The plane defined by three carbon atoms of the allyl group forms angles of 51.16 • and 38.79 • with those of the bicyclic system indole and the phenyl ring (C9-C14) attached to it, respectively.…”