Antitumor agents among indole sulfonamide derivatives

Chachoyan, A. A.; Shkulev, V. A.; Samvelyan, K. G.; Garibdzhanyan, B. T.; Papayan, G. L.

doi:10.1007/bf00764459

Cited by 2 publications

(3 citation statements)

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“…They obtained and studied diazaadamantanes ( 17 ), ( 100–110 ) ( Fig. 10 ) that contained fragments of substituted indoles and showed their high antitumor activity [ 46 ].…”

Section: Biological Activity Of Azaadamantanesmentioning

confidence: 99%

“…The most active compounds were also studied in mice with sarcomas 180 and 37. The therapeutic effect of the compounds was evaluated by the percentage of tumor growth inhibition (TGI, %) and compared with the effectiveness of the previously studied 5-(dimethylaminosulfonyl)-indole-3-carboxylic acid ( 111 ) [ 46 ] and 5,7‑dimethyl-6-oxo-1,3-diazaadamantane hydrochloric acid ( 21 ). A single therapeutic dose for each compound was assessed as ~1/20 of LD 100 .…”

Section: Biological Activity Of Azaadamantanesmentioning

confidence: 99%

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Azaadamantanes, a New Promising Scaffold for Medical Chemistry

et al. 2021

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Azaadamantanes are nitrogen-containing analogs of adamantane, which contain one or more nitrogen atoms instead of carbon atoms. This substitution leads to several specific chemical and physical properties. The azaadamantane derivatives have less lipophilicity compared to their adamantane analogs, which affects both their interaction with biological targets and bioavailability. The significant increase in the number of publications during the last decade (2009–2020) concerning the study of reactivity and biological activity of azaadamantanes and their derivatives indicates a great theoretical and practical interest in these compounds. Compounds with pronounced biological activity have been already discovered among azaadamantane derivatives. The review is devoted to the biological activity of azaadamantanes and their derivatives. It presents the main methods for the synthesis of di- and triazaadamantanes and summarizes the accumulated data on studying the biological activity of these compounds. The prospects for the use of azaadamantanes in medical chemistry and pharmacology are discussed.

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“…They obtained and studied diazaadamantanes ( 17 ), ( 100–110 ) ( Fig. 10 ) that contained fragments of substituted indoles and showed their high antitumor activity [ 46 ].…”

Section: Biological Activity Of Azaadamantanesmentioning

confidence: 99%

Section: Biological Activity Of Azaadamantanesmentioning

confidence: 99%

Azaadamantanes, a New Promising Scaffold for Medical Chemistry

et al. 2021

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“…The reaction of 1 with epichlorohydrin in DMSO in the presence of NaOH gives bi-1H-indole -3-carbaldehyde (54) on cooling [116] (Scheme 34). NaOH for 2 days gave bi-indole aldehyde (55) and tri-indole aldehyde (56), respectively [117,118] (Scheme 35).…”

Section: Bi and Tri-(1h-indole-3-carbaldehyde)mentioning

confidence: 99%