Structural Modifications of Nature-Inspired Indoloquinolines: A Mini Review of Their Potential Antiproliferative Activity

Abstract

Cryptolepine, neocryptolepine and isocryptolepine are naturally occurring indoloquinoline alkaloids with various spectrum of biological properties. Structural modification is an extremely effective means to improve their bioactivities. This review enumerates several neocryptolepine and isocryptolepine analogues with potent antiproliferative activity against MV4-11 (leukemia), A549 (lung cancer), HCT116 (colon cancer) cell lines in vitro. Its activity towards normal mouse fibroblasts BALB/3T3 was also evaluated. Furthermore, structure activity relationships (SAR) are briefly discussed. The anticancer screening of neocryptolepine derivatives was performed in order to determine their cytotoxic and growth inhibitory activities across the JFCR39 cancer cell line panel.

In Vitro and In Vivo Antitumor Activity of Indolo[2,3-b] Quinolines, Natural Product Analogs from Neocryptolepine Alkaloid

“…The alkaloid, neocryptolepine I or 5-methyl-indolo[3,2-b] quinoline, was isolated recently [ 6 , 7 , 8 ] showed antibacterial, antischistosomicidal, anticancer and antiplasmodial activity [ 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 ]. Further experiments indicated that the anticancer activity of indoloquinolines is based on DNA-binding, specifically by DNA base pair intercalation, followed by inhibition of the enzyme topoisomerase II [ 29 ].…”

Synthesis, characterization, and antibacterial activity of azodyes incorporated acridine chromophore and their applications in polyester printing

“…[9][10][11][12] Furthermore, acridines bearing rhodanine moiety and azo chromophore are important scaffold in broad spectrum activities in medicinal chemistry due to their diverse biological properties such as antimalarial, 13 antibacterial, 14 anticancer and DNA-intercalating agents. 15 The utilizing of Nheterocyclic such as acridine azo compounds allows them to bind with polyester textile fabrics by printing method is a hot point in an antibacterial test. These structures are an advantage by the presence of planner tricyclic fused aromatic system, and one or two flexible substituted pharmacophoric groups at different core position on the acridine skeleton.…”

Antitumoral Properties of Natural Products

“…In this Special Issue, six reviews were included aimed to summarize the antitumoral properties of different compounds isolated from several natural sources [36][37][38][39][40][41]. Liu et al reviewed the anticancer activities of the compounds porphyran and carrageenan, derived from red seaweed [36].…”

“…Possible mechanisms in the anticancer activity of these two polysaccharides were considered along with their possible cooperative actions with other anticancer chemotherapeutics [36]. Wang et al have reported a mini review on the anticancer activity of the naturally occurring indoloquinoline alkaloids cryptolepine, neocryptolepine, and isocryptolepine, isolated from the roots of Cryptolepis sanguinolenta and several of their analogues [37]. They presented an overview of the potential of neocryptolepine and isocryptolepine as scaffolds for the design and development of new anticancer drugs [37].…”

“…Wang et al have reported a mini review on the anticancer activity of the naturally occurring indoloquinoline alkaloids cryptolepine, neocryptolepine, and isocryptolepine, isolated from the roots of Cryptolepis sanguinolenta and several of their analogues [37]. They presented an overview of the potential of neocryptolepine and isocryptolepine as scaffolds for the design and development of new anticancer drugs [37]. Yang et al have reviewed diverse in vitro and in vivo pharmacological properties of capsazepine, a synthetic analogue of capsaicin (the common pungent ingredient of hot chili peppers) [38].…”