Antiproliferative Activity of N-Substituted 2,4-Diamino-5-Aryl-5,6,7,8,9,10-Hexahydrobenzo[B][1,8]Naphthyridine-3-Carbonitriles

doi:10.1007/s11094-020-02236-5

Paper

Antiproliferative Activity of N-Substituted 2,4-Diamino-5-Aryl-5,6,7,8,9,10-Hexahydrobenzo[B][1,8]Naphthyridine-3-Carbonitriles

Published Aug 1, 2020 · I. N. Bardasov, A. Y. Alekseeva, O. V. Ershov

Pharmaceutical Chemistry Journal

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Abstract

Th antiproliferative activity of N-substituted 2,4-diamino-5-aryl-5,6,7,8,9,10-hexahydrobenzo[b][1,8]naphthyridine-3-carbonitriles was studied. Substituents in the 5- and 7-positions of the naphthyridine ring had strong influences on the activity; in the 1-position, weak influences. Compounds with a C-5 3,4,5-trimethoxyphenyl radical were significantly superior to other derivatives. The influences of other substituents were not precisely established; however, a C-7 substituent played a key role in the manifestation of biological activity.

Study Snapshot

N-substituted 2,4-diamino-5-aryl-5,6,7,8,9,10-hexahydrobenzo[B][1,8]naphthyridine-3-carbonitriles show antiproliferative activity, with compounds with a

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Antiproliferative Activity of N-Substituted 2,4-Diamino-5-Aryl-5,6,7,8,9,10-Hexahydrobenzo[B][1,8]Naphthyridine-3-Carbonitriles

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References

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The structural modification of the 3,4,5-trimethoxyphenyl moiety in VERU-111, leading to a more potent antiproliferative agent, improves the potential for developing new antimitotic drugs.

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