Investigation of New Phenothiazine and Carbazole Derivatives as Potential Inhibitors of Human Farnesyltransferase

Phenothiazine-based CaaX competitive inhibitors of human farnesyltransferase bearing a cysteine, methionine, serine or valine moiety as a new family of antitumoral compounds

“…[1][2][3][4][5][6] FTase is a heterodimeric zinc metalloenzyme, responsible for posttranslational modification and activation of Ras proteins. Ras proteins undergo three sequential enzymatic posttranslational modifications.…”

Synthesis of hetero annulated isoxazolo-, pyrido- and pyrimido carbazoles: Screened for in vitro antitumor activity and structure activity relationships, a novel 2-amino-4-(3'-bromo-4'-methoxyphenyl)-8-chloro-11 H -pyrimido[4,5- a ]carbazole as an antitumor agent

“…Carbazoles and hetero annulated carbazole derivatives have attracted substantial attention due to their wide range of biological activities such as antidiabetic, antimicrobial, antioxidant, anticancer, antitubercular and anticonvulsant activity [9][10][11][12][13][14][15][16][17]. Many carbazole derivatives especially those with chloro substituents are important in the synthesis of new anti-cancer agents [18], and the carbazole back bone has been chosen here because it possess better inhibition properties compared to other nitrogen containing alkaloids.…”

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“…The synthesis of various hetero annulated carbazole derivatives has attracted substantial attention in recent years because there are several naturally occurring compounds that have similar structural frameworks, displaying a wide range of biological activities such as antioxidant, antidiabetic, antimicrobial, anticancer, antitubercular, antipsychotic and anticonvulsant activity [9][10][11][12][13][14][15][16][17] . It has been noticed that introduction of additional heterocyclic rings to the carbazole core tends to exert profound influence in increasing the anticancer activity.…”