Indoles are natural products which are well known for its anti-cancer activity due to its ability to induce cell death for many cancer cell lines. This review addresses indoles as natural products, mechanism of indoles, facilitated induction and recent studies with indoles and related compounds that were investigated via anti-cancer screening and that led to drug approval.
Various functionalised derivatives of 5H-cyclohepta [4,5]thieno [2,3-d][1,2,4]triazolo [4,3-a]pyrimidin-5-one were synthesised via reaction of hydrazonoyl halides (1) with either 1,2,3,5,6,7,8,9-octahydro-2-thioxo-4H-cyclohepta- [4,5]thieno [2,3-d]pyrimidin-4-one (2) or its methylthio derivative (3). The mechanism and the regioselectivity of the studied reactions are investigated and discussed.
Starting from 6-aryl-5-cyano-2-thiouracil derivative 1a-f, a series of novel thiazolo[3,2-a]pyrimidines 4a-f were synthesized. The mechanism and the regioselectivity of the studied reactions are discussed. In addition, a series of tetrahydro-4-H-pyrimido[2,1-b][1,3]thiazines 7a-e and 2-((ethoxymethyl)thio)-4-aryl-1,6-dihydropyrimidines 9b,c,e were synthesized. The anti-microbial activities of some of the prepared compounds were screened, and the results revealed that compounds 3c and 4c were more active than the standard (Ampicillin) against gram positive bacteria (Pseudomonas aeruginosa). Moreover, compounds 4b,e and 3f were found to be good antifungal agents against the studied fungal strains.
Substituted‐1,2,4‐triazines were conveniently synthesized in one pot by the cyclization of arylnitroformaldehyde hydrazone derivatives 1 and 5 with different primary amines in ~37% formaldehyde solution. The synthesized compounds were arranged into novel mono‐, bis‐, and tris‐nitro‐1,2,4‐triazine derivatives 2, 3, 4, 6, and 7. The antibacterial and antifungal activity of the synthesized compounds were screened against bacterial strains Escherichia coli (as Gram − ve) and Staphylococcus aureus (as Gram + ve), and fungal strains Aspergillus flavus and Candida albicans. All the synthesized compounds exhibit various patterns of inhibitory activity on the two pathogenic bacterial strains. However, the same compounds showed no activity against the tested fungal strains.
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